产品标题 产品货号 产品规格 厂家
4BP-TQSAxon 2694 CAS [360791-49-7] MF C18H17BrN2O2SMW 405.31 Purity: 99% Soluble in DMSO Description 4BP-TQS is an allosteric agonist of α7 nicotinic acetylcholine receptors (nAChR). The agonism was shown to act through a site topographically distinct from the ACh site. 4BP-TQS was a more potent and efficacious agonist of α7 nAChR than ACh (8-fold lower EC50 and 45-fold larger maximal response). The bioactive enantiomer of 4BP-TQS, GAT107 (Axon 2621), is also available. KEYWORDS: 4BP-TQS | supplier | α7 nAChR allosteric agonist | 4BPTQS | 4-BPTQS | 4-BP-TQS | CAS [360791-49-7] | Acetylcholine | nAChR | Allosteric agonist | Ion Channels | CAS [1476053-27-6]axonmedchem
GAT107Axon 2621 CAS [1476807-74-5] MF C18H17BrN2O2SMW 405.31 Purity: 99% Optical purity: >99% Soluble in DMSO Description GAT107, the bioactive enantiomer of 4BP-TQS (Axon 2694), is an allosteric agonist (EC50 value 28 μM) and positive allosteric modulator (PAM) of α7 nicotinic acetylcholine receptors. GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain. KEYWORDS: GAT107 | supplier | α7 nAChR agonist and PAM | GAT-107 | GAT 107 | CAS [1476807-74-5] | Acetylcholine | nAChR | Allosteric agonist | Ion Channelsaxonmedchem
AT 1001Axon 2401 CAS [1314801-63-2] MF C15H21BrN2MW 309.24 Purity: 100% Optical purity: Relative stereochemistry Soluble in 0.1N HCl(aq) and DMSO Description High affinity and selective α3β4 nAChR ligand (Ki value 2.6 nM at α3β4 nAChR) with both partial agonistic and antagonistic effects, and >90-fold selective over the other major subtypes, the α4β2 and α7 nAChR. AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding, and shows a mechanism of action very different from varenicline (Axon 1384 (HCl salt) and Axon 2074 (tartrate salt)). References Certificates Categories Extra info A. Cippitelli et al. AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol. 2015 Apr;172(7):1834-45.   L. Toll et al. AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats. Neuropsychopharmacology. 2012 May;37(6):1367-76.   E.W. Tuan et al. AT-1001 is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors. Mol Pharmacol. 2015 Jul 10. pii: mol.115.099978. [Epub ahead of print] Certificate of Analysis Material Safety Data Sheet CNS Pain & Inflammation nAChR Unclassified High affinity and selective α3β4 nAChR ligand with partial agonistic and antagonistic effects Chemical name N-(2-bromophenyl)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine Parent CAS No. [1314801-63-2] Order Size Unit Price Stock 10 mg €95.00 In Stockaxonmedchem
GTS 21 dihydrochloride - 3-(2,4-Dimethoxybenzylidene)-anabaseine dihydrochloride | DMXB | DMXB-AAxon 2860 CAS [156223-05-1] MF C19H20N2O2.2HClMW 381.30 Purity: 100% Soluble in water and DMSO Description Selective α7 nicotinic acetylcholine receptor (nAChR) partial agonist. At significantly higher concentrations GTS 21 behaves as an antagonist of α4β2 nAChRs and related type 3 5-HT receptors. KEYWORDS: GTS 21 dihydrochloride | supplier | α7 partial agonist | 3-(2 | 4-Dimethoxybenzylidene)-anabaseine dihydrochloride |  DMXB | DMXB-A | GTS21 | GTS-21 | CAS [156223-05-1] | [148372-04-7] | Acetylcholine | nAChR | Agonist | Ion Channels | α4β2 | 5-HT3axonmedchem
PHA 543613 dihydrochlorideAxon 2109 CAS [478148-58-2] MF C15H17N3O2.2HClMW 344.24 Purity: 99% Optical purity: Optically pure Soluble in water and DMSO Description Potent and selective α7 nicotinic acetylcholine receptor (nAChR) agonist, which is characterized by rapid brain penetration and high oral bioavailability; a potential treatment of cognitive deficits in schizophrenia References Certificates Categories Extra info DG Wishka et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive (...). J. Med. Chem. 2006, 49(14), 4425-4436.    PR Krafft et al. PHA-543613 Preserves Blood–Brain Barrier Integrity After Intracerebral Hemorrhage in Mice. Stroke, 2013, 44(6), 1743-1747.  Certificate of Analysis Material Safety Data Sheet CNS Pain & Inflammation nAChR Unclassified Pfizer Licensed Products nAChR agonist (α7 sub-unit selective) Chemical name (R)-N-(quinuclidin-3-yl)furo[2,3-c]pyridine-5-carboxamide dihydrochloride Source information Pfizer compound; Sold for research purposes under agreement from Pfizer Inc. Parent CAS No. [478149-53-0] Order Size Unit Price Stock 10 mg €115.00 In Stockaxonmedchem
Epibatidine dihydrochloride, (-)-Axon 1078 CAS [152378-30-8] MF C11H13ClN2.2HClMW 281.61 Purity: 99% Optical purity: 98% ee Soluble in water and DMSO Description Highly potent nicotinic agonist; (-)-Enantiomer of (±)-Epibatidine (Axon 1076).Its opposite enantiomer, (+)-Epibatidine (Axon 1077) is available as well. KEYWORDS: (-)-Epibatidine dihydrochloride | supplier | Nicotinic agonist | (-)-Epibatidine HCl | CAS [152378-30-8] | Acetylcholine | nAChR | Agonist | Ion Channels | Nicotine | receptor | Analgesic | Non-Narcotic | enantiomerically pureaxonmedchem
Epibatidine dihydrochloride, (+)-Axon 1077 CAS [166374-43-2] MF C11H13ClN2.2HClMW 281.61 Purity: 99% Optical purity: 99% ee Soluble in water and DMSO Description Highly potent nicotinic agonist; (+)-Enantiomer of (±)-Epibatidine (Axon 1076).Its opposite enantiomer, (-)-Epibatidine (Axon 1078) is available as well. KEYWORDS: (+)-Epibatidine dihydrochloride | supplier | Nicotinic agonist | (+)-Epibatidine HCl | CAS [166374-43-2] | [140111-52-0] | Acetylcholine | nAChR | Agonist | Ion Channels | Nicotine | receptor | Analgesic | Non-Narcotic | enantiomerically pureaxonmedchem
Epibatidine dihydrochloride, (±)-Axon 1076 CAS [162885-01-0] MF C11H13ClN2.2HClMW 281.61 Purity: 99% Soluble in water and DMSO Description Highly potent Nicotinic agonist, Analgesic, Non-Narcotic.The enantiopure (+)-Epibatidine (Axon 1077) and (-)-Epibatidine (Axon 1078) are available as well. KEYWORDS: (±)-Epibatidine dihydrochloride | supplier | Nicotinic agonist | Epibatidine HCl | CAS [162885-01-0] | [148152-66-3] | Acetylcholine | nAChR | Agonist | Ion Channel | Nicotine | receptor | Analgesic | Non-Narcoticaxonmedchem
BX 430Axon 2523 CAS [688309-70-8] MF C15H15Br2N3OMW 413.11 Purity: 99% Soluble in DMSO Description Noncompetitive, allosteric antagonist of human P2X4 receptor channels (IC50 value 0.54 μM as determined by Patch-clamp electrophysiology) with 10-100 fold selectivity over P2X1–P2X3, P2X5, and P2X7. A useful molecular probe to assess the specific role of P2X4 in inflammatory and neuropathic conditions, where ATP signaling has been shown to be dysfunctional. BX430 has no effect on mouse and rat P2X4Rs. KEYWORDS: BX 430 | supplier | P2X4 antagonist | BX430 | CAS [688309-70-8] | Calcium | P2X4 | Ion Channel | P2X | cation | inflammation | ATP | pain | purinoceptor | vasodilation | patch clamp | currentaxonmedchem
A 804598Axon 2182 CAS [1125758-85-1] MF C19H17N5MW 315.37 Purity: 99% Optical purity: >99% e.e. Soluble in DMSO Description Potent and selective P2X7 antagonist (IC50 values 10 nM, 9 nM, and 11 nM for rat, mouse, and human receptors respectively). A 804598 potently blocked agonist stimulated release of IL-1β and Yo-Pro uptake from differentiated THP-1 cells that natively express human P2X7 receptors.In another study, A 804598 was found to produce a concentration-dependent inhibition of BZ-ATP-stimulated calcium influx (IC50 value 28.71 nM) in cells expressing the rat recombinant P2X7 receptor; a useful tool for autoradiographic localization of P2X7 receptors in the rat brain and spinal cord. References Certificates Categories Extra info D.L. Donnelly-Roberts et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharm. 2009, 56, 223–229. S.L. Able et al. Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br. J. Pharmacol. 2011, 162, 405–414.  Certificate of Analysis Material Safety Data Sheet Apoptosis Cell Signaling & Oncology CNS Pain & Inflammation P2X7 Unclassified Potent and selective P2X7 antagonist Chemical name (S)-2-cyano-1-(1-phenylethyl)-3-(quinolin-5-yl)guanidine Parent CAS No. [1125758-85-1] Order Size Unit Price Stock 10 mg €125.00 In Stockaxonmedchem
GW 791343 hydrochlorideAxon 1967 CAS [309712-55-8] MF C20H24F2N4O.3HClMW 483.81 Purity: 98% Soluble in water and DMSO Description P2X7 receptor antagonist; GW791343 was a negative allosteric modulator of the human P2X(7) receptor but at the rat P2X(7) receptor its predominant effect was positive allosteric modulation References Certificates Categories Extra info AD Michel et al. Negative and positive allosteric modulators of the P2X(7) receptor. Br. J. Pharmacol. 2008, 153(4), 737-750.    AD Michel et al. Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects. Br. J. Pharmacol. 2008, 155(5), 7387-7351.  Certificate of Analysis Material Safety Data Sheet Apoptosis Cell Signaling & Oncology CNS Pain & Inflammation P2X7 Unclassified P2X7 receptor antagonist and allosteric modulator Chemical name 2-(3,4-difluorophenylamino)-N-(2-methyl-5-(piperazin-1-ylmethyl)phenyl)acetamide trihydrochloride Parent CAS No. [309712-73-0] Inquireaxonmedchem
JNJ 47965567Axon 2890 CAS [1428327-31-4] MF C28H32N4O2SMW 488.64 Purity: 99% Soluble in DMSO Description Highly potent and brain penetrant P2X7 antagonist in human, rat, and mouse cell lines (pKi values of 7.9, 7.9 and 6.9 for human, rat, and human whole blood P2X7). Probe compound for the preclinical assessment of P2X7 blockade in animal models of neuro-inflammation. DMPK properties suitable for preclinical pharmacodynamics studies. Keywords: JNJ 47965567 | supplier | P2X7 antagonist | JNJ47965567 | JNJ-47965567 | CAS [1428327-31-4] | Non Selective (Cations) | P2X7 | Antagonist | Ion Channels | Brain Penetrant | Neuro-inflammationaxonmedchem
Azasetron hydrochlorideAxon 1096 CAS [123040-16-4] MF C17H20ClN3O3.HClMW 386.27 Purity: 99% Soluble in water and DMSO Description Selective 5-HT3 antagonist. Enantiomerically pure forms of Azasetron HCl are available as well (Axon 2534 and Axon 2535 for (+)- and (-)-Azasetron, respectively). KEYWORDS: Azasetron hydrochloride | supplier | 5-HT3 antagonist | CAS [123040-16-4] | [123040-69-7] | Serotonin | 5-HT3 | Antagonist | Ion Channels | enantiomer | nausea | vomitting | cancer | chemotherapyaxonmedchem
Azasetron hydrochloride, (-)-Axon 2535 CAS [123040-96-0] MF C17H20ClN3O3.HClMW 386.27 Purity: 100% Optical purity: Optically pure Soluble in water and DMSO Description Selective 5-HT3 antagonist. (-)-enantiomer of Axon 1096 (racemic) KEYWORDS: (-)-Azasetron hydrochloride | supplier | 5-HT3 antagonist | CAS [123040-96-0] | [123040-95-9] | [123040-16-4] | [123040-69-7] | Serotonin | 5-HT3 | Antagonist | Ion Channels | enantiomer | nausea | vomitting | cancer | chemotherapyaxonmedchem
Granisetron hydrochloride - BRL 43694Axon 1449 CAS [107007-99-8] MF C18H24N4O.HClMW 348.87 Purity: 99% Soluble in water Description Serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy; water-soluble form References Certificates Categories Extra info Plosker and Goa. Granisetron. A review of its pharmacological properties and therapeutic use as an antiemetic. Drugs 1992, 42, 805.   Sanger and Nelson. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur. J. Pharmacol. 1989, 159, 113. Certificate of Analysis Material Safety Data Sheet CNS 5-HT3 Unclassified 5-HT3 antagonist Chemical name 1-methyl-N-((1R,3R,5S)-9-methyl-9-azabicyclo[3,3,1]nonan-3-yl)-1H-inzadole-3-carboxamide hydrochloride Parent CAS No. [109889-09-0] Order Size Unit Price Stock 25 mg €85.00 In Stockaxonmedchem
Alosetron hydrochlorideAxon 1097 CAS [122852-42-0] MF C17H18N4O.HClMW 330.81 Purity: 99% Soluble in water and DMSO Description Potent and selective 5-HT3 antagonist; a drug for irritable bowel syndrome (IBS) in women References Certificates Categories Extra info M Camilleri et al. Efficacy and safety of alosetron in women with irritable bowel syndrome: a randomised, placebo-controlled trial. Lancet. 2000 Mar 25;355(9209):1035-40. Certificate of Analysis Material Safety Data Sheet CNS 5-HT3 Unclassified 5-HT3 antagonist Chemical name 5-Methyl-2-(5-methyl-3H-imidazol-4-ylmethyl)-2,3,4,5-tetrahydro-pyrido[4,3-b]indol-1-one hydrochloride Parent CAS No. [122852-42-0] Order Size Unit Price Stock 10 mg €85.00 In Stockaxonmedchem
Azasetron hydrochloride, (+)-Axon 2534 CAS [123040-94-8] MF C17H20ClN3O3.HClMW 386.27 Purity: 100% Optical purity: Optically pure Soluble in water and DMSO Description Selective 5-HT3 antagonist. (+)-enantiomer of Axon 1096 (racemic) KEYWORDS: (+)-Azasetron hydrochloride | supplier | 5-HT3 antagonist | CAS [123040-94-8] | [123040-93-7] | [123040-69-7] | [123040-16-4] | Serotonin | 5-HT3 | Antagonist | Ion Channels | enantiomer | nausea | vomitting | cancer | chemotherapyaxonmedchem
ZQ-16Axon 2616 CAS [376616-73-8] MF C10H16N2O2SMW 228.31 Purity: 99% Soluble in DMSO and Ethanol Description Potent and selective small-molecule GPR84 agonist (EC50 value 0.139 µM in a calcium mobilization assay). ZQ-16 induced phosphorylation of ERK1/2, and a dose-dependent reduction of forskolin-stimulated cAMP accumulation in HEK293 cells expressing GPR84. KEYWORDS: ZQ-16 | supplier | GPR84 agonist | ZQ16 | CAS [376616-73-8] | FFA | GPR84 | GPCR | free fatty acids | ERK1 | ERK3 | inflammation | immunology | cAMPaxonmedchem
AR 420626Axon 2794 CAS [1798310-55-0] MF C21H18Cl2N2O3MW 417.29 Purity: 99% Soluble in DMSO Description AR 420626 is an allosteric FFA3 (GPR41) receptor agonist (pEC50 value of 5.74) which enhances mucosal defenses and prevents NSAID-induced enteropathy via the GLP-2 pathway in rats. KEYWORDS: AR 420626 | supplier | GPR41 agonist | AR420626 | AR-420626 | CAS [1798310-55-0] | FFA | GPR41 | Agonist | Receptors | FFA3 | GLP-2axonmedchem
AMG 837 calcium saltAxon 2405 CAS [1291087-14-3] MF C26H20F3O3.½CaMW 457.47 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Orally bioavailable partial agonist of the GPR40 (EC50 value 13.5 nM for AMG 837 stimulated Ca2+ flux in CHO cells expressing human GPR40) with a superior pharmacokinetic profile. AMG837 stimulated robust glucose-dependent insulin secretion (EC50 value 142±20 nM) in isolated rodent islets, and lowered post-prandial glucose in normal rats. AMG-837 exhibits a potential utility for the treatment of type 2 diabetes. References Certificates Categories Extra info D.C. Lin et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011;6(11):e27270.   J.B. Houze et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.   J. Luo et al. A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents. PLoS One. 2012;7(10):e46300.   Y.J. Choi et al. G-protein coupled receptor 40 agonists as novel therapeutics for type 2 diabetes. Arch Pharm Res. 2014 Apr;37(4):435-9. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Diabetes & Metabolism GPR40 A11 Orally bioavailable partial agonist of GPR40 (FFA1) Chemical name (S)-3-(4-((4'-(trifluoromethyl)biphenyl-3-yl)methoxy)phenyl)hex-4-ynoic acid calcium salt Parent CAS No. [865231-46-5] Order Size Unit Price Stock 5 mg €110.00 In Stockaxonmedchem
GSK 137647AAxon 2582 CAS [349085-82-1] MF C16H19NO3SMW 305.39 Purity: 99% Soluble in DMSO and Ethanol Description Potent FFA4/GPR120 agonist (pEC50 value 6.3 nM for hFFA4) with >100-fold selectivity over a panel of 65 targets including FFA1-FFA3. GSK137647A reproduces the secretion of active GLP-1 mediated by long-chain Fas (LCFAs), especially ALA.  KEYWORDS: GSK 137647A | FFA4/GPR120 agonist | GSK137647A | GSK-137647A | GSK137647 | CAS [349085-82-1] | FFA | GPR120 | Agonist | FFA4 | fatty acid | LCFA | metabolic | insulin | Type 2 | diabetes mellitus | inflammation | interleukin | ILaxonmedchem
TUG 891Axon 2075 CAS [1374516-07-0] MF C23H21FO3MW 364.41 Purity: 99% Soluble in DMSO Description Potent and selective agonist for G-protein coupled receptor 120 (GPR120), also known as the free fatty acid receptor FFA4 (EC50: 44 and 17 nM for human GPR120 and mouse GPR120 respectively KEYWORDS: TUG 891 | supplier | GPR120 agonist | TUG891 | CAS [1374516-07-0] | FFA | GPR120 | Agonist | Receptorsaxonmedchem
GW 9508Axon 2013 CAS [885101-89-3] MF C22H21NO3MW 347.41 Purity: 100% Soluble in 0.1N NaOH(aq) and DMSO Description Potent and selective agonist for the free fatty acid receptor FFA1 (GPR40) References Certificates Categories Extra info CP Briscoe et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br. J. Pharmacol. 2006, 148(5), 619-628.    T Fujita et al. A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. J. Invest. Dermatol. 2011, 131(8), 1660-1667.  Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Diabetes & Metabolism GPR40 A11 GPR40 receptor agonist (FFA1) Chemical name 3-(4-(3-phenoxybenzylamino)phenyl)propanoic acid Parent CAS No. [885101-89-3] Order Size Unit Price Stock 10 mg €85.00 In Stockaxonmedchem
D3-βArr - NCGC 00379308Axon 2895 CAS [662164-09-2] MF C20H23N5MW 333.43 Purity: 99% Soluble in DMSO Recently addedaxonmedchem
HMR 1031Axon 1616 CAS [479203-71-9] MF C35H41N5O6MW 627.73 Purity: 98% Optical purity: Optically pure Soluble in DMSO and Ethanol Description Potent and specific integrin α4β1 or very late antigen 4 (VLA-4) receptor antagonist binding to vascular cell adhesion molecule-1 (VCAM-1) and fibronectin; HMR1031 is a potential inhaled drug for the treatment of asthma References Certificates Categories Extra info B Shah et al. Effect of food on pharmacokinetics of an inhaled drug: a case study with a VLA-4 antagonist, HMR1031. J. Clin. Pharmacol. 2003, 43(12), 1341-9.   S Rohatagi et al. Pharmacoscintigraphic comparison of HMR 1031, a VLA-4 antagonist, in healthy volunteers following delivery via a nebulizer and a dry powder inhaler. Am. J. Ther. 2004, 11(2), 103-113.   Z Diamant et al. Effect of a very late antigen-4 receptor antagonist on allergen-induced airway responses and inflammation in asthma. Clin. Exp. Allergy 2005, 35(8), 1080–1087.  Certificate of Analysis Material Safety Data Sheet Immunology Pain & Inflammation VLA-4 Receptor VCAM VLA-4 antagonist Chemical name (S)-3-((S)-2-(4,4-dimethyl-2,5-dioxo-3-(4-(3-o-tolylureido)benzyl)imidazolidin-1-yl)-4-methylpentanamido)-3-phenylpropanoic acid Parent CAS No. [479203-71-9] Order Size Unit Price Stock 2 mg €105.00 In Stockaxonmedchem
FedovapagonAxon 2146 CAS [347887-36-9] MF C27H34N4O3MW 462.58 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Potent and selective vasopressin V2 receptor agonist (EC50 of 24 nM); demonstrated positive anti-diuretic effect in nocturia References Certificates Categories Extra info CM Yea et al. New Benzylureas as a Novel Series of Potent, Nonpeptidic Vasopressin V2 Receptor Agonists. J. Med. Chem. 2008, 51(24), 8124-8134.   I Tsukamoto. Recent patenting activities in the discovery and development of vasopressin V2 receptor agonists. Exp. Opin. Ther. Patents. 2012, 22(6), 579-586.   Certificate of Analysis Material Safety Data Sheet Cardiovascular CNS A6 Vasopressin (V) Selective vasopressin V2 receptor agonist Chemical name (S)-N2,N2-dimethyl-N1-(2-methyl-4-(2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)benzyl)pyrrolidine-1,2-dicarboxamide Parent CAS No. [347887-36-9] Order Size Unit Price Stock 5 mg €135.00 In Stockaxonmedchem
Tolvaptan - OPC 41061Axon 1591 CAS [150683-30-0] MF C26H25ClN2O3MW 448.94 Purity: 99% Soluble in DMSO Description A highly potent, oral and selective antagonist of vasopressin V2 receptor References Certificates Categories Extra info Y Yamamura et al. OPC-41061, a Highly Potent Human Vasopressin V2-Receptor Antagonist: Pharmacological Profile and Aquaretic Effect by Single and Multiple Oral Dosing in Rats. J. Pharmacol. Exp. Ther. 1998, 287(3), 860-867.    T Hirano et al. Effects of the V2-Receptor Antagonist OPC-41061 and the Loop Diuretic Furosemide Alone and in Combination in Rats. JPET 2000, 292(1), 288-294.     RW Schrier et al. Tolvaptan, a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia. N Engl J Med 2006, 355, 2099-2112.  Certificate of Analysis Material Safety Data Sheet Cardiovascular CNS A6 Vasopressin (V) Vasopressin (V2) antagonist Chemical name N-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide Parent CAS No. [150683-30-0] Order Size Unit Price Stock 10 mg €105.00 In Stockaxonmedchem
SR 49059 - RelcovaptanAxon 1256 CAS [150375-75-0] MF C28H27Cl2N3O7SMW 620.50 Purity: 98% Optical purity: Optically pure Soluble in DMSO Description Highly potent and selective vasopressin V1A receptor antagonist. KEYWORDS: SR 49059 | supplier | V1A antagonist | Relcovaptan | SR49059 | CAS [150375-75-0] | Vasopressin | Vasopressin (V) | Antagonist | Receptorsaxonmedchem
SSR 149415 - NelivaptanAxon 1114 CAS [439687-69-1] MF C30H32ClN3O8SMW 630.11 Purity: 99% Optical purity: >98% ee Soluble in DMSO Description Selective and orally active non-peptide antagonist of vasopressin V1b receptor (Ki values 91 nM and 1.5 nM for V1a and V1b in human CHO cells, respectively); a potential drug for treatment of anxiety and depression. KEYWORDS: SSR 149415 | supplier | V1B antagonist | Nelivaptan | SSR149415 | SSR-149415 | CAS [439687-69-1] | Vasopressin | GPCR | anxiety | depression | orally activeaxonmedchem
Vasopressin antagonist 1867 - Compound 12iAxon 1867 CAS [909391-88-4] MF C28H36N4O4MW 492.61 Purity: 99% Soluble in 0.1N HCl(aq) and DMSO Description Orally available and selective V1b receptor antagonist (IC50 value 3 nM for hV1b inhibition, exhibiting >1000-fold selectivity over hV1a, hV2, and hOT). A useful tool to study Vasopressin 1B receptor pharmacology. KEYWORDS: Vasopressin antagonist 1867 | supplier | V1b antagonist | Compound 12i | CAS [909391-88-4] | Vasopressin | orally available | hypothalamic | pituitary | adrenal | HPA-axis | corticotrophin | neuroendocrine | antidepressant | anxiolytic | MSD | Akzo Nobelaxonmedchem
P2Y14 Antagonist Prodrug 7j hydrochlorideAxon 1958 CAS [1315308-19-0] MF C33H31F3N2O3.HClMW 597.07 Purity: 98% Soluble in water and DMSO Description Prodrug of P2Y14 receptor antagonist; highly bioavailable References Certificates Categories Extra info J Robichaud et al. Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14). Bioorg. Med. Chem. Lett. 2011, 21(14), 4366-4368. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology P2Y14 A12 Prodrug of P2Y14 receptor antagonist Chemical name 2-(dimethylamino)-2-oxoethyl 4-(4-(piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate hydrochloride Parent CAS No. [1315308-19-0] Order Size Unit Price Stock 5 mg €125.00 In Stockaxonmedchem
Eltrombopag - SB 497115Axon 1872 CAS [496775-61-2] MF C25H22N4O4MW 442.47 Purity: 98% Soluble in 0.1N NaOH(aq) and DMSO Description First-in-class, oral, nonpeptide thrombopoietin receptor (TpoR or MPL) agonist, which is developed as a treatment for thrombocytopenia of various etiologies. Eltrombopag activates TpoR signaling pathway and induces proliferation and differentiation in mammalian cells and cell lines References Certificates Categories Extra info JM Jenkins et al. Phase 1 clinical study of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist. Blood 2007, 109 (11), 4739–4741.    JB Bussel et al. Eltrombopag for the treatment of chronic idiopathic thrombocytopenic purpura. N. Engl. J. Med. 2007, 357(22), 2237-2247.    CL Erickson‐Miller et al. Preclinical Activity of Eltrombopag (SB‐497115), an Oral, Nonpeptide Thrombopoietin Receptor Agonist. Stem Cells 2009, 27(2), 424-430. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Stem Cell TPO (c-MPL) Unclassified Stem Cell Differentiator Thrombopoietin receptor (TpoR or c-MPL) agonist Chemical name (Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxybiphenyl-3-carboxylic acid Parent CAS No. [496775-61-2] Order Size Unit Price Stock 5 mg €95.00 In Stockaxonmedchem
MRS 2578Axon 1862 CAS [711019-86-2] MF C20H20N6S4MW 472.67 Purity: 99% Soluble in DMSO Description Potent and selective P2Y6 nucleotide receptor antagonist References Certificates Categories Extra info LK Mamedova et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol. 2004, 67(9), 1763-1770.    S Koizumi et al. UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis. Nature 2007, 446(7139), 1091-1095.  Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology P2Y6 A11 P2Y6 nucleotide receptor antagonist Chemical name 1,1'-(butane-1,4-diyl)bis(3-(3-isothiocyanatophenyl)thiourea) Parent CAS No. [711019-86-2] Order Size Unit Price Stock 10 mg €90.00 In Stockaxonmedchem
Calhex 231 hydrochlorideAxon 1818 CAS [N.A.] MF C25H27ClN2O.HClMW 443.41 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Negative allosteric modulator (NAM) of the extracellular Calcium-sensing receptor (CaSR or CaR); inhibit Ca2+-induced accumulation of [3H]inositol phosphates in HEK293 cells (IC50: 0.39 microm) References Certificates Categories Extra info C Petrel et al. Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca(2+)-sensing receptor. J. Biol. Chem. 2003, 278(49), 49487-49494.   A Kessler et al. N1-Benzoyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (calhex 231) as a new calcium sensing receptor ligand (...). J. Med. Chem. 2006, 49(17), 5119-5128.  Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology CNS CaSR C1 NAM of the extracellular CaSR Chemical name 4-chloro-N-((1S,2S)-2-((R)-1-(naphthalen-1-yl)ethylamino)cyclohexyl)benzamide hydrochloride Parent CAS No. [652973-93-8] Order Size Unit Price Stock 5 mg €99.00 In Stockaxonmedchem
CaSR antagonist 18cAxon 1732 CAS [802916-30-9] MF C32H35N3O6MW 557.64 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Calcium-sensing receptor (CaSR) antagonist (IC50: 76 nM); potential anabolic agent for the treatment of osteoporosis References Certificates Categories Extra info W Yang et al. Discovery and Structure−Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists. J. Med. Chem. 2009, 52(4), 1204–1208. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology CNS CaSR C1 Calcium-sensing receptor (CaSR) antagonist Chemical name (S)-6-(1-hydroxy-3-phenylpropan-2-ylamino)-N-(2-phenoxyethyl)-2-(3,4,5-trimethoxyphenyl)nicotinamide Parent CAS No. [802916-30-9] Order Size Unit Price Stock 5 mg €125.00 In Stockaxonmedchem
C-DIM12 - DIM-C-pPhClAxon 2575 CAS [178946-89-9] MF C23H17ClN2MW 356.85 Purity: 99% Soluble in DMSO Description Potent and specific Nurr1 activator that stimulates Nurr1 mediated apoptosis axis in bladder cancer cells and tumors and inhibits NF-κB–dependent gene expression in glial cells by stabilizing nuclear corepressor proteins, which reduces binding of p65 to inflammatory gene promoters. C-DIM12 protects against loss of dopamine neurons in the substantia nigra as well as dopamine terminals in the striatum in MPTP-induced mouse models for Parkinson's disease. KEYWORDS: C-DIM12 | supplier | Nurr1 activator | DIM-C-pPhCl | CDIM12 | C-DIM 12 | CAS [178946-89-9] | Intracellular Transcription Factors | NURR | Activator | Nuclear Receptors | NR4A2 | inflammation | CNS | dopaminergic | neurons | NF-κB | ganglia | Parkinson'saxonmedchem
C-DIM8 - DIM-C-pPhOHAxon 2827 CAS [151358-47-3] MF C23H18N2OMW 338.40 Purity: 98% Soluble in DMSO Description C-DIM8 is a Nur77 (NR4A1) antagonist. Treatment of pancreatic and colon cancer cells with C-DIM8 mimics the effects of NR4A1 knockdown and decreases β1-integrin expression, β1-integrin regulated genes and responses including migration and adhesion. KEYWORDS: C-DIM8 | supplier | Nur77 antagonist | DIM-C-pPhOH | CDIM8 | CAS [151358-47-3] | Intracellular Transcription Factors | Nurr | Antagonist | Receptors | TRAILaxonmedchem
C-DIM5 - DIM-C-pPhOCH3Axon 2828 CAS [33985-68-1] MF C24H20N2OMW 352.43 Purity: 99% Soluble in DMSO Description C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival, induction of apoptosis, induced expression of the apoptosis gene/protein TRAIL, and inhibited tumor growth in vivo. C-DIM5 induces G0-G1–phase to S-phase arrest in Panc1 cells, and this is accompanied by Nur77-dependent induction of the cyclin-dependent kinase inhibitor p21. KEYWORDS: C-DIM5 | supplier | Nur77 agonist | DIM-C-pPhOCH3 | CDIM5 | CAS [33985-68-1] | Intracellular Transcription Factors | Nurr | Agonist | Receptors | TRAILaxonmedchem
NVP-BHG712 - BHG 712Axon 1829 CAS [940310-85-0] MF C26H20F3N7OMW 503.48 Purity: 98% Soluble in DMSO Description Potent and specific inhibitor of EphB4 kinase References Certificates Categories Extra info G Martiny-Baron et al. The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis. Angiogenesis. 2010, 13(3), 259-267. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Pain & Inflammation EphB4 RTK class XIII; EV 2.7.10.1 Inhibitor of EphB4 kinase Chemical name 4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide Parent CAS No. [940310-85-0] Order Size Unit Price Stock 2 mg €85.00 In Stockaxonmedchem
AX-024 hydrochlorideAxon 2692 CAS [1704801-24-0] MF C21H22FNO2.HClMW 375.86 Purity: 99% Soluble in water and DMSO Description First-in-class inhibitor of T cell receptor (TCR); AX-024 is an orally available inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 value 1 nM). By modulating TCR signaling, the inhibitor prevented the development of psoriasis and asthma and, furthermore, exerted a long-lasting therapeutic effect in a model of autoimmune encephalomyelitis. KEYWORDS: AX-024 hydrochloride | supplier | T cell receptor inhibitor | AX024 hydrochloride | AX 024 hydrochloride | AX-024 | AX024 | AX 024 | Ax24 | CAS [1704801-24-0] | [1370544-73-2] | Antigen | T cell | Inhibitor | Receptors | TCR | Autoimmune | Nck | TCR-Nck | Psoriasis | Asthma | Encephalomyelitisaxonmedchem
FPS-ZM1Axon 2858 CAS [945714-67-0] MF C20H22ClNOMW 327.85 Purity: 99% Soluble in DMSO Description FPS-ZM1 is a high-affinity RAGE-specific inhibitor (Ki value of 25 nM) which binds specifically to the V domain of RAGE, crosses the BBB, and inhibits Aβ-induced cellular stress in RAGE-expressing cells in vitro and in brain in vivo. FPS-ZM1 was not toxic to cells and mice. KEYWORDS: FPS-ZM1 | supplier | RAGE inhibitor | FPS ZM1 | FPSZM1 | CAS [945714-67-0] | AGE | RAGE | Inhibitor | Receptors | Alzheimer's disease | Amyloid β peptide | Aβaxonmedchem
DJ-V-159Axon 2942 CAS [2253744-53-3] MF C24H12F6N4O2MW 502.37 Purity: 99% Soluble in DMSO Recently addedaxonmedchem
AR 244555Axon 2191 CAS [858350-62-6] MF C23H23ClF2N2OMW 416.89 Purity: 99% Soluble in 0.1N HCl(aq) and DMSO Description Inverse agonist of Mas G-protein signaling (IC50 values 186 and 348 nM in human and rat inositol phosphatase (IP) Gq coupling assays respectively). AR 244555 caused a dose-dependent inhibition of inositol 1,4,5-trisphosphate accumulation in AdMas-infected cells, and attenuated the sarcomeric organization and cell enlargement observed in Mas overexpressing myocytes.AR 244555 caused a modest but significant increase in coronary flow in rat hearts witout causing arrhythmias, and provides protection from ischemia-reperfusion injury if administered either before ischemia or immediately before reperfusion. References Certificates Categories Extra info T. Zhang et al. Inhibition of Mas G-protein signaling improves coronary blood flow, reduces myocardial infarct size, and provides long-term cardioprotection. Am. J. Physiol. Heart Circ. Physiol. 2012, 302, H299-311.  Certificate of Analysis Material Safety Data Sheet Angiogenesis Cardiovascular Cell Signaling & Oncology Mas A8 Inverse agonist of Mas G-protein signaling Chemical name (1'-(but-3-enyl)-5-chlorospiro[indoline-3,4'-piperidine]-1-yl)(2,6-difluorophenyl)methanone Parent CAS No. [858350-62-6] Order Size Unit Price Stock 5 mg €125.00 In Stockaxonmedchem
APD 597 - JNJ 38431055Axon 2541 CAS [897732-93-3] MF C21H29N5O6SMW 479.55 Purity: 99% Soluble in DMSO Description Orally bioavailable selective GPR119 agonist (EC50 value 44 nM for hGPR119, IC50 value 13 μM) with a good balance between agonist potency, intrinsic activity, metabolic profile and in particular on its good solubility and reduced drug–drug interaction potential. In clinical trial, JNJ 38431055 was well tolerated and not associated with hypoglycaemia. KEYWORDS: APD 597 | supplier | GPR119 agonist | JNJ 38431055 | APD597 | JNJ38431055 | CAS [897732-93-3] | [897732-74-0] | Cannabinoids | GPR119 | Agonist | diabetes melitus | T2DM |  insulin | incretin | glucose | glucagon | cAMPaxonmedchem
APD 668 - JNJ 28630368Axon 2380 CAS [832714-46-2] MF C21H24FN5O5SMW 477.51 Purity: 100% Soluble in DMSO Description Potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat. APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM). References Certificates Categories Extra info G. Semple et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg. Med. Chem. Lett. 2011, 21, 3134-3141.   M. Sakairi et al. Synthesis and pharmacological profile of a new selective G protein-coupled receptor 119 agonist; 6-((2-fluoro-3-(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)propyl)amino)-2,3-dihydro.... Chem. Pharm. Bull. 2012, 60, 1093-1095.   E. Weisberg et al. Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One. 2013, 8, e56473. Certificate of Analysis Material Safety Data Sheet CNS Diabetes & Metabolism Endocrinology GPR119 A15 Potent and selective, orally active GPR119 agonist Chemical name isopropyl 4-(1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate Parent CAS No. [832714-46-2] Order Size Unit Price Stock 5 mg €125.00 In Stockaxonmedchem
M 24 - M024/C21Axon 1969 CAS [477775-14-7] MF C23H29N3O4S2MW 475.62 Purity: 98% Soluble in DMSO Description First reported non-peptide selective AT2 receptor agonist (Ki 0.4nM and 10.000 nM for AT2 and AT1 respectively). M 24 shows a bioavailability of 20-30% after oral administration and a half-life estimated to 4 h in rat. Note:axonmedchem
MBX 2982Axon 2092 CAS [1037792-44-1] MF C22H24N8OSMW 448.54 Purity: 98% Soluble in DMSO Description Potent and selective agonist of G-protein coupled receptor 119 (GPR119); an orally active agent to treat type 2 diabetes; MBX 2982 acts directly on the β cell to increase insulin secretion. In addition, it stimulates release of the incretin GLP-1 from the gut References Certificates Categories Extra info J Seewoodhary and SC Bain. Novel treatments for type 2 diabetes. Br. J. Gen. Pract. 2011, 61(582): 5–6.    RM Jones et al. GPR119 agonists for the treatment of type 2 diabetes. Exp. Opin. Ther. Pat. 2009, 19(10), 1339-1359.  Certificate of Analysis Material Safety Data Sheet CNS Diabetes & Metabolism Endocrinology GPR119 A15 Potent and selective GPR119 agonist Chemical name 4-((4-(1H-tetrazol-1-yl)phenyl1H-tetrazol-1-yl)phenoxy)methyl)-2-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)thiazole Parent CAS No. [1037792-44-1] Order Size Unit Price Stock 5 mg €125.00 In Stockaxonmedchem
AR 231453Axon 1572 CAS [733750-99-7] MF C21H24FN7O5SMW 505.52 Purity: 99% Soluble in DMSO Description Potent and orally active agonist of cannabinoid receptor GPR119. KEYWORDS: AR 231453 | supplier | GPR119 agonist | AR231453 | AR-231453 | CAS [733750-99-7] | Cannabinoids | GPR119 | Agonist | Receptorsaxonmedchem
PD 123319 ditrifluoroacetateAxon 1276 CAS [136676-91-0] MF C31H32N4O3.2C2HF3O2MW 736.66 Purity: 99% Optical purity: Optically pure Soluble in water and DMSO Description Angiotensin II (AT-2) antagonist KEYWORDS: PD 123319 ditrifluoroacetate | supplier | AT2 antagonist | PD123319 | PD0123319 | CAS [136676-91-0] | [130663-39-7] | Angiotensin II | Antagonist | AT-II | cardiovascular | renalaxonmedchem
BETP - Compound BAxon 2259 CAS [1371569-69-5] MF C20H17F3N2O2SMW 406.42 Purity: 99% Soluble in DMSO Description Positive allosteric modulator (PAM) at the glucagon-like peptide 1 receptor (GLP-1; EC50 value 0.66 μM) with good selectivity over GLP-2, GIP, PTH, and glucagon receptors. BETP has a signifficant effect on cAMP accumulation, iCa2+ mobilization, and β-arrestin1 and β-arrestin2 recruitment in Flp-In-CHO cells stably expressing the human GLP-1R (pEC50 values 5.2, 5, 5.0, and 5.0, respectively). BETP induced glucose-dependent insulin secretion in vitro and in vivo, and increased calcium influx in CHO cells expressing GLP-1R. References Certificates Categories Extra info D. Wootten et al. Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands. Mol. Pharmacol. 2013, 83, 822-834.   F.S. Willard et al. Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin. Mol. Pharmacol. 2012, 82, 1066-10673.   Y.H. Cheong et al. Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently. Biochem. Biophys. Res. Commun. 2012, 417, 558-563.   K.W. Sloop et al. Novel small molecule glucagon-like peptide-1 receptor agonist stimulates insulin secretion in rodents and from human islets. Diabetes. 2010, 59, 3099-3107. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Diabetes & Metabolism Endocrinology GLP-1 B1 Positive allosteric modulator (PAM) at the GLP-1 receptor Chemical name 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine Parent CAS No. [1371569-69-5] Order Size Unit Price Stock 10 mg €105.00 In Stockaxonmedchem
 |< < 28 29 30 31 32 33 34 > >| 第 32/34 页