| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| GLP-1R agonist DMB - DMB | Axon 1907
CAS [281209-71-0]
MF C13H15Cl2N3O2SMW 348.25
Purity:
99%
Soluble in DMSO
Description
Glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonist; potential agent for the treatment of type 2 diabetes; a usuful tool for studying the role of GLP-1 in both in vivo and in vitro diabetes and obesity models
References
Certificates
Categories
Extra info
LB Knudsen et al. Small molecule agonists for the glucagon-like peptide-1 receptor. Proc. Natl. Acad. Sci. USA, 2007, 104(3), 937-942. (*compound 2 in this article)
C Koole et al. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner; implications for drug screening. Mol. Pharmacol. 2010, 78(3), 456-465.
N Irwin et al. Insulin-releasing and metabolic effects of small molecule GLP-1 receptor agonist 6,7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline. Eur. J. Pharmacol. 2010, 1-3, 268-273.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Endocrinology
GLP-1
B1
GLP-1 Receptor (GLP1R) Agonist
Chemical name
N-tert-butyl-6,7-dichloro-3-(methylsulfonyl)quinoxalin-2-amine
Parent CAS No.
[281209-71-0]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| AZ-GHS-22 | Axon 2340
CAS [1143020-91-0]
MF C27H33ClN6O5S2MW 621.17
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally available high affinity Ghrelin receptor (GHS-R1a) inverse agonist (IC50 0.77 nM) with very low CNS exposure.
KEYWORDS: AZ-GHS-22 | supplier | GHS-R1a inverse agonist | AZGHS22 | CAS [1143020-91-0] | Metabolism | GHSR | Inverse agonist | Ghrelin | CNS | food | intake | metabolism | brain penetrant | | axonmedchem |
| Chloro-DPAT hydrochloride, 6- | Axon 1068
CAS [1246094-87-0]
MF C16H24ClN.HClMW 302.28
Purity:
98%
Soluble in water
Description
Bioactive tetralin derivative
References
Certificates
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Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
Bioactive tetralin derivative
Chemical name
(6-Chloro-1,2,3,4-tetrahydro-naphthalen-2-yl)-dipropyl-amine hydrochloride
Parent CAS No.
[1246242-29-4]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| BI 6015 | Axon 1940
CAS [93987-29-2]
MF C15H13N3O4SMW 331.35
Purity:
99%
Soluble in DMSO
Description
Potent hepatocyte nuclear factor 4α (HNF4α) antagonist; found to be selectively cytotoxic to cancer cell lines in vitro and in vivo
References
Certificates
Categories
Extra info
A Kiselyuk et al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem. Biol. 2012, 19(7), 806-818.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
HNF4α
NR2A
Potent hepatocyte nuclear factor 4α (HNF4α) antagonist
Chemical name
2-methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole
Parent CAS No.
[93987-29-2]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| GLP-1 antagonist | Axon 1132
CAS [475466-57-0]
MF C28H37N3O3MW 463.61
Purity:
99%
Soluble in DMSO
Description
Glucagon-like peptide-1 (GLP-1) receptor antagonist
References
Certificates
Categories
Extra info
XS He et al. Neurogen Co. US6482844B1 (Nov 19, 2002).
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Endocrinology
GLP-1
B1
GLP-1 Receptor Antagonist
Chemical name
N-[4,5-Dimethyl-1-(2-methyl-benzyl)-1H-imidazol-2-ylmethyl]-2,4-dimethoxy-N-(3-methyl-butyl)-benzamide
Parent CAS No.
[475466-57-0]
Order
Size
Unit Price
Stock
5 mg
€150.00
In Stock | | axonmedchem |
| MK 677 - Ibutamoren mesylate | L 163191 | MK 0677 | Axon 1376
CAS [159752-10-0]
MF C27H36N4O5S.CH4O3SMW 624.77
Purity:
99%
Optical purity:
Optically pure
Soluble in water
Description
Potent and orally active growth hormone (GH) secretagogue; high affinity Ghrelin receptor agonist.
KEYWORDS: MK 677 | supplier | GH secretagogue | Ibutamoren mesylate | L 163191 | MK 0677 | MK677 | MK0677 | L163191 | CAS [159752-10-0] | [159634-47-6] | Metabolism | GHSR | Agonist | Ghrelin | growth hormone | | axonmedchem |
| CpdD hydrochloride - GhrR antagonist CpdD | Axon 2147
CAS [N.A.]
MF C25H33BrN4O3S.HClMW 585.98
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Selective ghrelin receptor (GhrR aka GHSR-1a) antagonist
References
Certificates
Categories
Extra info
KA Longo et al. Pharmacologic inhibition of ghrelin receptor signaling is insulin sparing and promotes insulin sensitivity. J. Pharmacol. Exp. Ther. 2011, 339(1), 115-124.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Endocrinology
A7
Ghrelin (GHSR)
Ghrelin receptor (GhrR aka GHSR-1a) antagonist
Chemical name
(R)-N-(1-(3-(4-bromobenzyl)-1,2,4-oxadiazol-5-yl)-3-phenylpropyl)-3-(diethylamino)propane-1-sulfonamide hydrochloride
Parent CAS No.
[916984-47-9]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| EMPA | Axon 2012
CAS [680590-49-2]
MF C23H26N4O4SMW 454.54
Purity:
99%
Soluble in DMSO and Ethanol
Description
Highly potent and selective orexin type 2 (OX2) receptor antagonist, with Ki values of >900 and 1 nM for OX1 and OX2 receptors respectively
References
Certificates
Categories
Extra info
P Malherbe et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br. J. Pharmacol. 2009, 156, 1326–1341.
TE Scammell and CJ Winrow. Orexin Receptors: Pharmacology and Therapeutic Opportunities. Annu. Rev. Pharmacol. Toxicol. 2011. 51:243–66.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Endocrinology
A6
Orexin (OX)
Orexin type 2 (OX2) receptor antagonist
Chemical name
N-ethyl-2-(N-(6-methoxypyridin-3-yl)-2-methylphenylsulfonamido)-N-(pyridin-3-ylmethyl)acetamide
Parent CAS No.
[680590-49-2]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Dilept - GZR 123 | Axon 1975
CAS [200954-39-8]
MF C21H30N2O5MW 390.47
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N NaOH(aq) and DMSO
Description
Neurotensin (NT) and dopamine (DA) receptor antagonist; dipeptide neuroleptic of potential efficacy in relieving positive and negative symptoms of schizophrenia
References
Certificates
Categories
Extra info
MV Retyunskaya et al. Neuromodulatory mechanism underlying the effect of the atypical dipeptide neuroleptic dilept. Bull. Exp. Biol Med. 2003, 136(5), 467-470.
RU Ostrovskaia et al. Dilept: a tripeptoid neurotensin analog combining neuroleptic activity with positive mnemotropic action. Eksp. Klin. Farmakol. 2005, 68(1), 3-6.
RU Ostrovskaia et al. Neurotensine dipeptide analog dilept decreases the deficiency of prestimulus startle reflex inhibition: a prognostic sign of antipsychotic activity. Eksp. Klin. Farmakol. 2009, 72(5), 3-7.
Certificate of Analysis
Material Safety Data Sheet
CNS
D2
D3
A17
A7
Neurotensin (NT)
Neurotensin and dopamine receptor antagonist
Chemical name
(S)-methyl 2-((S)-1-hexanoylpyrrolidine-2-carboxamido)-3-(4-hydroxyphenyl)propanoate
Parent CAS No.
[200954-39-8]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| TCS1102 | Axon 2744
CAS [916141-36-1]
MF C27H26N4O2SMW 470.59
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
TCS1102 is a potent and selective dual orexin receptor antagonist (Ki values of 3 and 0.2 nM for hOX1R and hOX2R, respectively). Moreover, TCS1102 demonstrated in vivo central activity when dosed peripherally in a pharmacodynamic model of orexin activity.
KEYWORDS: TCS1102 | supplier | OX1/2 antagonist | TCS 1102 | TCS-1102 | DORA-1 | DORA1 | DORA 1 | CAS [916141-36-1] | Orexin | Orexin (OX) | Antagonist | Receptors | | axonmedchem |
| SR 142948 | Axon 1255
CAS [184162-64-9]
MF C39H51N5O6MW 685.85
Purity:
98%
Soluble in water
Description
Neurotensin (NT) receptor antagonist; orally active in vivo.
KEYWORDS: SR 142948 | supplier | NT antagonist | SR142948 | CAS [184162-64-9] | Neurotensin | Neurotensin (NT) | Antagonist | Receptors | | axonmedchem |
| SR 48692 - Meclinertant | Axon 1164
CAS [146362-70-1]
MF C32H31ClN4O5MW 587.07
Purity:
99%
Low solubility in organic solvents
Description
An orally active, non-peptide, high affinity neurotensin (NT1 or NTS1) receptor antagonist.
KEYWORDS: SR 48692 | supplier | NT1 antagonist | Meclinertant | SR48692 | CAS [146362-70-1] | Neurotensin | NT | NTS1 | cocaine sensitization | nitric oxide | diuretic action | | axonmedchem |
| SB 674042 | Axon 2192
CAS [483313-22-0]
MF C24H21FN4O2SMW 448.51
Purity:
99%
Optical purity:
>99% ee
Soluble in DMSO and Ethanol
Description
Nonpeptide OX1 selective antagonist (Kd value 3.76 nM) with >100 fold selectivity over the OX2 receptor. SB 674042 displays no significant affinity for a range of serotonergic, dopaminergic, adrenergic and purinergic receptors at concentrations up to 10 μM.
SB 674042 was also shown to be a competitive, functional antagonist of the OX1 receptor in the calcium mobilisation assay using CHO-DG44_OX1 cell lines.
References
Certificates
Categories
Extra info
A. Heifetz et al. Study of Human Orexin-1 and -2 G-Protein-Coupled Receptors with Novel and Published Antagonists by Modeling, Molecular Dynamics Simulations, and Site-Directed Mutagenesis. Biochem. 2012, 51, 3178-3197.
C.J. Langmead et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br. J. Pharmacol. 2004, 141, 340-346.
P. Malherbe et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br. J. Pharmacol. 2009, 156, 1326-1341.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Endocrinology
A6
Orexin (OX)
Nonpeptide OX1 selective antagonist with >100 fold selectivity over the OX2 receptor.
Chemical name
(S)-(5-(2-fluorophenyl)-2-methylthiazol-4-yl)(2-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)pyrrolidin-1-yl)methanone
Parent CAS No.
[483313-22-0]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| SB 334867 | Axon 2095
CAS [792173-99-0]
MF C17H13N5O2MW 319.32
Purity:
99%
Soluble in DMSO
Description
First selective orexin type 1 (OX1) receptor antagonist; Its affinity for OX1R is ~50-fold higher than for OX2R
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Endocrinology
A6
Orexin (OX)
First selective orexin 1 (OX1) antagonist
Chemical name
1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
Parent CAS No.
[792173-99-0]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| ML314 | Axon 2632
CAS [1448895-09-7]
MF C24H28N4O3MW 420.50
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Brain penetrant nonpeptidic β-Arrestin biased full agonist of the neurotensin NTR1 receptor (EC50 values 2.0 μM and >80 µM for NTR1 and NTR2, respectively). Unlike peptide-based NTR1 agonists, ML314 has no significant response in a Ca2+ mobilization assay. ML314 is a viable, preclinical lead for methamphetamine abuse treatment.
KEYWORDS: ML314 | supplier | NTR1 agonist | ML-314 | CAS [1448895-09-7] | Neurotensin | GPCR | drug abuse | allosteric | β-arrestin | dopamine | CNS | BBB | | axonmedchem |
| ICI 192605 | Axon 1210
CAS [117621-64-4]
MF C22H23ClO5MW 402.87
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
A potent and selective, orally active thromboxane A2 (TP) receptor antagonist
References
Certificates
Categories
Extra info
Al-Jarad et al. Effects of a thromboxane receptor antagonist on prostaglandin D2 and histamine induced bronchoconstriction in man. Br. J. Clin. Pharmacol. 1994, 37, 97.
Shaw et al. Combined administration of 5-HT2 and thromboxane A2 antagonists: effects on platelet aggregation and isolated cardiac muscle. Br. J. Pharmacol.1997, 121(5), 875–882.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Thromboxane A2
A14
Thromboxane A2 antagonist
Chemical name
(Z)-6-[(2S,4S,5R)-2-(2-Chloro-phenyl)-4-(2-hydroxy-phenyl)-[1,3]dioxan-5-yl]-hex-4-enoic acid (relative stereochemistry)
Parent CAS No.
[117621-64-4]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| Hydroxybuspirone hydrochloride, (S)-6- - BMS 442606 hydrochloride | Axon 1998
CAS [N.A.]
MF C21H31N5O3.HClMW 437.96
Purity:
99%
Soluble in water and DMSO
Description
Optically pure (S)-enantiomer of 6-hydroxybuspirone (Axon 1996), a major active metabolite of Buspirone (Axon 1995); 5-HT1A partial agonist. (S)-Enantiomer has advantage of being cleared more slowly from blood compared to the (R)-enantiomer; while (R)-Enantiomer showed higher affinity and selectivity for the 5HT1A receptor compared to the (S)-enantiomer
References
Certificates
Categories
Extra info
H Wong et al. 6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. Drug Metab. Dispos. 2007, 35(8), 1387-1392.
RC Dockens et al. Pharmacokinetics of 6-hydroxybuspirone and its enantiomers administered individually or following buspirone administration in humans. Biopharm. Drug Dispos. 2007, 28(7), 393-402.
SJ Nicholson et al. Development of oral extended release formulations of 6-hydroxybuspirone. Biopharm. Drug Dispos. 2012, 33(9), 522-535.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A partial agonist
Chemical name
(S)-6-hydroxy-8-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride
Parent CAS No.
[477930-31-7]
Order
Size
Unit Price
Stock
1 mg
€105.00
In Stock | | axonmedchem |
| Hydroxy-DPAT hydrobromide, (S)-(-)-8- - DPAT, (S)-(-)-8-OH- | Axon 1017
CAS [78095-20-2]
MF C16H25NO.HBrMW 328.29
Purity:
98%
Optical purity:
98% ee
Soluble in DMSO
Description
5-HT1A receptor partial agonist, less active enantiomer of (±)-8-OH-DPAT (Axon 1015), in comparison with R-(+)-8-hydroxy-DPAT (Axon 1016) as a full 5-HT1A agonist
References
Certificates
Categories
Extra info
T Yoshitake and J Kehr. Differential effects of (R)-, (R, S)- and (S)-8-hydroxy-2-(di-n-propylamino)tetralin on hippocampal serotonin release and induction of hypothermia in awake rats. Life Sci. 2004, 74, 2865.
LJ Cornfield et al. Intrinsic activity of enantiomers of 8-hydroxy-2-(di-n-propylamino)tetralin and its analogs at 5-hydroxytryptamine1A receptors that are negatively coupled to adenylate cyclase. Mol. Pharmacol. 1991, 39, 780.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A agonist
Chemical name
(S)-7-Dipropylamino-5,6,7,8-tetrahydro-naphthalen-1-ol hydrobromide
Parent CAS No.
[80300-10-3]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Hydroxybuspirone hydrochloride, (R)-6- - BMS 442608 hydrochloride | Axon 1997
CAS [N.A.]
MF C21H31N5O3.HClMW 437.96
Purity:
99%
Soluble in water and DMSO
Description
Optically pure (R)-enantiomer of 6-hydroxybuspirone (Axon 1996), a major active metabolite of Buspirone (Axon 1995); 5-HT1A partial agonist. (R)-Enantiomer showed higher affinity and selectivity for the 5HT1A receptor compared to the (S)-enantiomer; while (S)-Enantiomer has advantage of being cleared more slowly from blood compared to the (R)-enantiomer
References
Certificates
Categories
Extra info
H Wong et al. 6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. Drug Metab. Dispos. 2007, 35(8), 1387-1392.
RC Dockens et al. Pharmacokinetics of 6-hydroxybuspirone and its enantiomers administered individually or following buspirone administration in humans. Biopharm. Drug Dispos. 2007, 28(7), 393-402.
SJ Nicholson et al. Development of oral extended release formulations of 6-hydroxybuspirone. Biopharm. Drug Dispos. 2012, 33(9), 522-535.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1A
A19
5-HT1A partial agonist
Chemical name
(R)-6-hydroxy-8-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-8-azaspiro[4.5]decane-7,9-dione hydrochloride
Parent CAS No.
[477930-30-6]
Order
Size
Unit Price
Stock
1 mg
€105.00
In Stock | | axonmedchem |
| JNJ 63533054 | Axon 2569
CAS [1802326-66-4]
MF C17H17ClN2O2MW 316.78
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, brain-penetrant, orally active, and selective agonist of hGPR139 (EC50 value 16 nM; 138% of max) with no inhibitory effect on CYP450. A useful tool for exploring GPR139 pharmacology, especially when combined with NCRW0005-F05 (Axon 2609), the first potent GPR139 antagonist available.
KEYWORDS: JNJ 63533054 | supplier | GPR139 agonist | JNJ63533054 | CAS [1802326-66-4] | GPR139 | Agonist | GPCR | orphan | CNS | diabetes | metabolic | brain | tool | central nervous system | | axonmedchem |
| CID 1375606 | Axon 2915
CAS [313493-80-0]
MF C20H14Cl2N2O2MW 385.24
Purity:
98%
Soluble in DMSO
Description
CID 1375606 is a selective surrogate agonist for GPR27 (pEC50 value of 6.34 for GPR27V2).
KEYWORDS: CID 1375606 | supplier | GPR27 agonist | CID1375606 | CID-1375606 | CAS [313493-80-0] | Non Selective | GPR27 | Agonist | Receptors | SREB1 | β-Arrestin 2 | | axonmedchem |
| NCRW0005-F05 | Axon 2609
CAS [342779-66-2]
MF C16H13F2NO2MW 289.28
Purity:
99%
Soluble in DMSO
Description
First antagonist selective for GPR139 (IC50 value 0.21 µM); a useful tool to study GPR139 pharmacology, especially in combination with the GPR139 agonist JNJ 63533054 (Axon 2569)
KEYWORDS: NCRW0005-F05 | supplier | GPR139 antagonist | NCRW0005F05 | CAS [342779-66-2] | GPR139 | GPCR | orphan | CNS | Gαq | G-alphaq | diabetes | obesity | Parkinson’s | | axonmedchem |
| LY 334370 hydrochloride | Axon 1612
CAS [199673-74-0]
MF C21H22FN3O.HClMW 387.88
Purity:
99%
Soluble in water and DMSO
Description
Selective 5-HT1F receptor agonist with Ki value to be 1.87 nM
References
Certificates
Categories
Extra info
DS Dupuis et al. G-protein activation at 5-HT1A receptors by the 5-HT1F ligand LY-334,370 in guinea-pig brain sections and recombinant cell lines. Br. J. Pharmacol. 1998, 124(2), 283–90.
S Shepheard et al. Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY-334,370. Cephalalgia 1999, 19(10), 851-858.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT1F
A19
5-HT1F antagonist
Chemical name
4-fluoro-N-(3-(1-methylpiperidin-4-yl)-1H-indol-5-yl)benzamide hydrochloride
Parent CAS No.
[182563-08-2]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Org OD 02-0 - 19-CH2P4 | Axon 2085
CAS [13258-85-0]
MF C22H30O2MW 326.47
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO
Description
Selective agonist of membrane progesterone receptor (mPR; IC50 value 33.9 nM). Org OD 02-0 mimics the protective effects of progestin hormones on serum starvation-induced cell death and apoptosis in both granulosa and breast cancer cells without altering caspase 3 activity. Org OD 02-0 significantly increased mitochondrial membrane potential (MMP) in serum starved MB468 cells.
KEYWORDS: Org OD 02-0 | supplier | mPR agonist | 19-CH2P4 | OrgOD02-0 | 19-CH2P4 | CAS [13258-85-0] | Progesterone | Progesterone (mPR) | Agonist | Receptors | Progestin | membrane | adipoQ | PAQR | | axonmedchem |
| Seratrodast - AA 2414 | Axon 1447
CAS [112665-43-7]
MF C22H26O4MW 354.44
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Thromboxane A2 (TP) receptor antagonist used in the treatment of asthma
References
Certificates
Categories
Extra info
S Endo and K Akiyama. Thromboxane A2 receptor antagonist in asthma therapy (in Japanese). Nippon Rinsho 54 (11): 3045–8.
S Hada et al. Study on the inhibitory effect of AA-2414 on platelet aggregation and its clinical effect in asthmatic patients (in Japanese). Arerugi 42 (1): 18–25.
Kurokawa et al. Antagonism of the human thromboxane A2 receptor by an anti-asthmatic agent AA-2414. Biol.Pharm.Bull. 1994, 17, 383.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Immunology
Pain & Inflammation
Thromboxane A2
A14
Thromboxane A2 antagonist
Chemical name
7-Phenyl-7-(2,4,5-trimethyl-3,6-dioxo-cyclohexa-1,4-dienyl)-heptanoic acid
Parent CAS No.
[112665-43-7]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| SB 699551A | Axon 1469
CAS [791789-61-2]
MF C34H45N3O.2HClMW 584.66
Purity:
99%
Soluble in DMSO
Description
Selective 5-HT5A receptor antagonist
References
Certificates
Categories
Extra info
DF Corbett et al. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg. Med. Chem. Letts. 2005, 15, 4014.
DR Thomas et al. SB-69951-A , a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain. Neuropharmacology 2006, 51, 566.
DR Thomas. 5-ht5A receptors as a therapeutic target. Pharmacol. Ther. 2006, 111, 707.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT5A
A19
5-HT5A antagonist
Chemical name
3-Cyclopentyl-N-(2-dimethylamino-ethyl)-N-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-propionamide dihydrochloride
Parent CAS No.
[864741-95-7]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| SR 27897 - Lintitript | Axon 1245
CAS [136381-85-6]
MF C20H14ClN3O3SMW 411.86
Purity:
99%
Soluble in DMSO
Description
Potent and selective CCK1 antagonist
References
Certificates
Categories
Extra info
Gully et al. Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors. Eur. J. Pharmacol. 1993, 23, 232.
Poncelet M. Et al. Neurobehavioural effects of SR 27897, a selective cholecystokinin type A (CCK-A) receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 1993, 348(1), 102-107.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Miscellaneous
Pain & Inflammation
CCK1
Endocrinology
A6
CCK1 antagonist
Chemical name
{2-[4-(2-Chloro-phenyl)-thiazol-2-ylcarbamoyl]-indol-1-yl}-acetic acid
Parent CAS No.
[136381-85-6]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| T 98475 | Axon 1270
CAS [199119-18-1]
MF C37H37F2N3O4SMW 657.77
Purity:
98%
No solubility data
Description
Potent and orally active antagonist of Gonadotropin releasing hormone (GnRH), also known as luteinising hormone releasing hormone (LHRH)
References
Certificates
Categories
Extra info
Sarma et al. Peptidomimetic GnRH receptor antagonists for the treatment of reproductive and proliferative diseases. Expert Opinon on Ther. Patent. 2006, 16(6), 733-751.
Cho et al. Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J. Med. Chem. 1998, 41, 4190.
Cell Signaling & Oncology
CNS
GnRH
Endocrinology
A6
GnRH or LHRH antagonist
Chemical name
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-isobutyrylamino-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid isopropyl ester
Parent CAS No.
[199119-18-1]
Inquire | | axonmedchem |
| SB 268262 | Axon 1145
CAS [217438-17-0]
MF C18H15N3O4S2MW 401.46
Purity:
99%
Soluble in DMSO
Description
Selective non-peptide CGRP1 antagonist; racemate of (+)-SB-273779
References
Certificates
Categories
Extra info
N Aiyar et al. Pharmacology of SB-273779, a Nonpeptide Calcitonin Gene-Related Peptide 1 Receptor Antagonist. J. Pharmacol. Exp. Ther. 2001, 296, 768–775.
Certificate of Analysis
Material Safety Data Sheet
CNS
CGRP1
B1
CGRP1 antagonist
Chemical name
N-Methyl-3-nitro-4-(thiazole-2-sulfinyl)-N-o-tolyl-benzamide
Parent CAS No.
[217438-17-0]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| SB 269970 hydrochloride - SB 269970A | Axon 2183
CAS [261901-57-9]
MF C18H28N2O3S.HClMW 388.95
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent and selective 5-HT7 antagonist (pKi value 8.9 for 5-HT7a) with >50 fold selectivity over a wide range of serotonergic, dopaminergic and adrenergic receptors. Analogue of SB 258741 hydrochloride (Axon 1100). SB 269970 significantly blocked amphetamine and ketamine-induced hyperactivity and reversed amphetamine-induced but not ketamine-induced prepulsed inhibiton (PPI) deficits, without changing spontaneous locomotor activity and startle amplitude.
References
Certificates
Categories
Extra info
P.J. Lovell et al. A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970). J. Med. Chem. 2000, 43, 342-345.
R. Galici et al. Effects of SB-269970, a 5-HT7 receptor antagonist, in mouse models predictive of antipsychotic-like activity. Behav. Pharmacol. 2008, 19, 153-159.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
5-HT7
A19
Potent and selective 5-HT7 antagonist
Chemical name
(R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidin-1-ylsulfonyl)phenol hydrochloride
Parent CAS No.
[201038-74-6]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| ML 221 | Axon 2870
CAS [877636-42-5]
MF C17H11N3O6SMW 385.35
Purity:
99%
Soluble in DMSO
Description
Potent apelin (APJ) receptor functional antagonist in cell-based assays (IC50 value is 1.75 µM). ML 221 is >37-fold selective over the closely related angiotensin II type 1 (AT-1) receptor.
KEYWORDS: ML 221 | supplier | APJ antagonist | ML221 | ML-221 | CAS [877636-42-5] | Apelin | Apelin (APJ) | Antagonist | Receptors | | axonmedchem |
| ML 154 - NCGC 00185684 | NCGC 84 | Axon 2321
CAS [1345964-89-7]
MF C29H26N2PS.BrMW 545.47
Purity:
99%
Soluble in DMSO
Description
Competitive, selective, and brain penetrant NPS receptor antagonist that preferentially blocks NPS-induced ERK phosphorylation over intracellular Ca2+ or cAMP responses (IC50 values 22.1 nM, 36.5 nM, and 5.0 nM, in Ca2+, cAMP, and binding assays, respectively). NCGC84 decreases alcohol self-administration in vivo, and does not inhibit the vasopressin V1b or the endogenous purinergic receptor at concentrations up to 10 µM.
References
Certificates
Categories
Extra info
A. Thorsell et al. A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant.... J Neurosci. 2013 Jun 12;33(24):10132-42. doi: 10.1523/JNEUROSCI.4742-12.2013.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
A6
NPSR
Competitive, selective, and brain penetrant NPS receptor antagonist
Chemical name
1-cinnamyl-3-(diphenylphosphorothioyl)-2-methyl-1H-imidazo[1,2-a]pyridin-4-ium bromide
Parent CAS No.
[1346105-73-4]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| MK 0354 | Axon 1576
CAS [851776-28-8]
MF C7H8N6MW 176.18
Purity:
99%
Soluble in DMSO
Description
Partial agonist of Niacin receptor, G-protein coupled receptor 109a
References
Certificates
Categories
Extra info
E Lai et al, Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans. J. Clin. Lipidol. 2008, 2(5), 375-383.
G Semple et al. 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice. JMC. 2008, 51(16), 5101.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
GPR109a
A11
GPR109a partial agonist; affects HDL levels in blood
Chemical name
3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole
Parent CAS No.
[851776-28-8]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| SB 258741 hydrochloride | Axon 1100
CAS [N.A.]
MF C19H30N2O2S.HClMW 386.98
Purity:
99%
Optical purity:
>98% ee
Soluble in water
Description
Serotonin 5-HT7 antagonist.
KEYWORDS: SB 258741 hydrochloride | supplier | 5-HT7 antagonist | SB258741 | CAS [201038-58-6] | Serotonin | 5-HT7 | Antagonist | Receptors | | axonmedchem |
| EPPTB - RO 5212773 | Axon 2419
CAS [1110781-88-8]
MF C20H21F3N2O2MW 378.39
Purity:
100%
Soluble in DMSO
Description
The first, highly potent and selective full antagonist of the trace amine-associated receptor 1 (TAAR1; IC50 value 28 nM at mouse TAAR1). EPPTB blocks the TAAR1-mediated activation of an inwardly rectifying K+ channels. A useful pharmacological tool for in vitro and in vivo investigations to study the role of TAAR1 in psychiatric and neurodegenerative disorders.
References
Certificates
Categories
Extra info
H. Stalder et al. Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773). Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31.
A. Bradaia et al. The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6.
Certificate of Analysis
Material Safety Data Sheet
CNS
A17
TAAR1
The first, highly potent and selective full antagonist of TAAR1
Chemical name
N-(3-ethoxyphenyl)-4-(pyrrolidin-1-yl)-3-(trifluoromethyl)benzamide
Parent CAS No.
[1110781-88-8]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| BT-11 | Axon 2749
CAS [1912399-75-7]
MF C30H24N8O2MW 528.56
Purity:
99%
Soluble in DMSO
Description
BT-11 is a first-in-class, orally active lanthionine synthetase C-like 2 (LANCL2) binding compound (Kd value of 7.7 µM) for treating inflammatory bowel disease (IBD). Moreover, BT-11 downregulates expression of pro-inflammatory cytokines (e.g., TNF-α or interferon-γ, which are hallmarks of IBD), and promotes IL-10-mediated anti-inflammatory responses in the GI tract.
KEYWORDS: BT-11 | supplier | LANCL2 modulator | BT11 | BT 11 | CAS [1912399-75-7] | Abscisic acid | LANCL | Modulator | Receptors | IBD | | axonmedchem |
| Ambrisentan - BSF 208075 | Letairis | Volibris | Axon 1648
CAS [177036-94-1]
MF C22H22N2O4MW 378.42
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Orally active non-peptide endothelin-A (ETA) receptor antagonist; therapeutic agent for the treatment of pulmonary arterial hypertension
References
Certificates
Categories
Extra info
H Vatter and V Seifert. Ambrisentan, a non-peptide endothelin receptor antagonist. Cardiovasc Drug Rev 2006, 24 (1), 63–76.
CC Chong. Ambrisentan: A new, nonsulphonamide, selective endothelin receptor antagonist for the treatment of pulmonary arterial hypertension. PVRI Review 2009, 1, 31-33.
H Riechers et al. Discovery and Optimization of a Novel Class of Orally Active Nonpeptidic Endothelin-A Receptor Antagonists. J. Med. Chem., 1996, 39(11), 2123–2128.
Certificate of Analysis
Material Safety Data Sheet
CNS
ETA
Endocrinology
A7
Endothelin-A (ETA) antagonist
Chemical name
(S)-2-(4,6-dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropanoic acid
Parent CAS No.
[177036-94-1]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| ML329 - CID 12387471 | Axon 2733
CAS [19992-50-8]
MF C16H12N2O4SMW 328.34
Purity:
99%
Soluble in DMSO
Description
ML329 is an inhibitor of the MITF molecular pathway (IC50 value of 1.2 μM; TRPM-1 promoter activity) and showed specific activity against MITF-dependent cells (IC50 values of 0.1 and 0.7 μM in SK-MEL-5 and MALME-3M cell lines, respectively). ML329 also reduced the expression of the cell cycle regulator CDK2, and showed CDK1 inhibition (IC50 value of 0.5 μM).
KEYWORDS: ML329 | supplier | MITF inhibitor | CID 12387471 | ML 329 | ML-329 | CAS [19992-50-8] | DNA-RNA | MITF | Inhibitor | Transcription Factors | Microphthalmia-associated transcription factor | Melanoma | | axonmedchem |
| Aminotetraline hydrochloride, (S)-5-Methoxy-N-propyl-2- | Axon 1027
CAS [93601-86-6]
MF C14H21NO.HClMW 255.78
Purity:
98%
Optical purity:
>98% ee
No solubility data
Description
Dopamine receptor agonist
References
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Categories
Extra info
CNS
D2
D3
D4
D1
A17
Dopamine agonist
Chemical name
((S)-5-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-amine hydrochloride
Parent CAS No.
[101403-24-1]
Inquire | | axonmedchem |
| SB 207499 - Cilomilast | Ariflo | Axon 1592
CAS [153259-65-5]
MF C20H25NO4MW 343.42
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Selective and orally active inhibitor of phosphodiesterase-4 (PDE4); a potential agent for the treatment of respiratory disorders such as asthma and Chronic Obstructive Pulmonary Disease (COPD); a second generation PDE4 inhibitor, reduces tumor necrosis factor α and interleukin-4 production in vivo
References
Certificates
Categories
Extra info
TJ Torphy et al. Ariflo (SB 207499), a second generation phosphodiesterase 4 inhibitor for the treatment of asthma and COPD: from concept to clinic. Pulmonary Pharmacol. Ther. 1999, 12(2), 131-135.
H Ochiai et al. Highly potent PDE4 inhibitors with therapeutic potential. Bioorg. Med. Chem. Lett. 2004, 14(1), 207-210.
SB Christensen et al. 1,4-Cyclohexanecarboxylates: Potent and Selective Inhibitors of Phosophodiesterase 4 for the Treatment of Asthma. J. Med. Chem. 1998, 41(6), 821.
DE Griswold etal. SB 207499 (Ariflo), a Second Generation Phosphodiesterase 4 Inhibitor, Reduces Tumor Necrosis Factor α and Interleukin-4 Production in vivo. J. Pharmacol. Exp. Ther. 1998, 287(2), 705-711.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.53
PDE
PDE4 inhibitor
Chemical name
4-Cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
Parent CAS No.
[153259-65-5]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Bromomethyl-1-(tetrahydro-pyran-2-yl)-1H-indazole, 5- | Axon 1177
CAS [368426-64-6]
MF C13H15BrN2OMW 295.18
Purity:
97%
No solubility data
Description
Key precursor for making e.g. non-covalent thrombin inhibitors
References
Certificates
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Extra info
Non Selective
Building Block; unknown pharmacology
Chemical name
5-Bromomethyl-1-(tetrahydro-pyran-2-yl)-1H-indazole
Parent CAS No.
[368426-64-6]
Inquire | | axonmedchem |
| Chloro-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo[2,3-d]pyrimidine, 4- | Axon 1117
CAS [157286-81-2]
MF C17H18ClN3MW 299.80
Purity:
98%
No solubility data
Description
Building Block
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Non Selective
Building Block; unknown pharmacology
Chemical name
4-Chloro-2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidine
Parent CAS No.
[157286-81-2]
Inquire | | axonmedchem |
| Chloro-4-(methylthio)-benzeneacetic acid methyl ester, 3- | Axon 1295
CAS [436141-65-0]
MF C10H11ClO2SMW 230.71
Purity:
98%
No solubility data
Description
Building Block
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Non Selective
Building Block; unknown pharmacology
Chemical name
(3-Chloro-4-methylsulfanyl-phenyl)-acetic acid methyl ester
Parent CAS No.
[436141-65-0]
Inquire | | axonmedchem |
| Chloro-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one, 2- | Axon 2866
CAS [2241432-81-3]
MF C13H8ClFN2OMW 262.67
Purity:
99%
Recently added | | axonmedchem |
| Chloropurine riboside, 6- - Chloropurine 9-β-D-ribofuranoside | NSC 4910 | Axon 2417
CAS [5399-87-1]
MF C10H11ClN4O4MW 286.67
Purity:
98%
Optical purity:
Optically pure
N.A.
Description
Useful building block in the synthesis of 6-substituted purine ribosides
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Non Selective
Building block in the synthesis of 6-substituted purine ribosides
Chemical name
(2R,3S,4R,5R)-2-(6-chloro-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol
Parent CAS No.
[5399-87-1]
Order
Size
Unit Price
Stock
1000 mg
€75.00
In Stock | | axonmedchem |
| Methyl-3-cyclopentyl-2-(4-methylsulfonylphenyl)propionate | Axon 1135
CAS [300355-19-5]
MF C16H22O4SMW 310.41
Purity:
97%
No solubility data
Description
Building Block
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Non Selective
Building Block; unknown pharmacology
Chemical name
3-Cyclopentyl-2-(4-methanesulfonyl-phenyl)-propionic acid methyl ester
Parent CAS No.
[300355-19-5]
Inquire | | axonmedchem |
| Methylthioadenosine, 2- - Adenosine, 2-MeS- | NSC 36900 | Axon 1192
CAS [4105-39-9]
MF C11H15N5O4SMW 313.33
Purity:
97%
No solubility data
Description
Adenosine precursor for 2-MeS-ATP or 2-MeS-ADP or 2-MeS-AMP
References
Certificates
Categories
Extra info
R.A. Proctor et al. Protection of mice from endotoxic death by 2-methylthio-ATP. Proc. Natl. Acad. Sci. U S A. 1994, 91, 6017-6020.
Non Selective
Building Block; unknown pharmacology
Chemical name
(2R,3R,4S,5R)-2-(6-Amino-2-methylsulfanyl-purin-9-yl)-5-hydroxymethyl-tetrahydro-furan-3,4-diol
Parent CAS No.
[4105-39-9]
Inquire | | axonmedchem |
| Propionic acid, 2-[4-(Cyclopropylsulfonyl)phenyl]-3-(tetrahydropyran-4-yl) | Axon 1284
CAS [745052-93-1]
MF C17H22O5SMW 338.42
Purity:
98%
No solubility data
Description
Building Block; Unknown pharmacology
References
Certificates
Categories
Extra info
Non Selective
Building Block; unknown pharmacology
Chemical name
2-(4-Cyclopropanesulfonyl-phenyl)-3-(tetrahydro-pyran-4-yl)-propionic acid
Parent CAS No.
[745052-93-1]
Inquire | | axonmedchem |
| K+ Channel inhibitor 1734 | Axon 1734
CAS [343240-54-0]
MF #N/AMW #N/A
Purity:
97%
Optical purity:
racemate
Soluble in DMSO and Ethanol
Description
Building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur). The ethylester analog of inhibitor 1734 is a modest inhibitor itself (IC50 value 1.1 µM for human Kv1.5), but exhibiting encouraging KV1.5 versus L-type calcium channel selectivity.
KEYWORDS: K+ Channel inhibitor 1734 | supplier | Building block | CAS [343240-54-0] | [1026960-80-4] | Potassium | Kv1.5 | Ikur | BMS | L-type | calcium channel | | axonmedchem |
| 3-Chloro-4-(pyridin-3-yl)-1,2,5-thiadiazole | Axon 2592
CAS [131986-28-2]
MF C7H4ClN3SMW 197.64
Purity:
99%
N.A.
Description
Useful building block for the synthesis of FP-TZTP
KEYWORDS: 3-Chloro-4-(pyridin-3-yl)-1,2,5-thiadiazole | supplier | Building block | CAS [131986-28-2] | FP-TZTP | [18F]-FP-TZTP | muscarinic | M2 | PET | precursor | positron emission tomography | | axonmedchem |