| 产品详情 |
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| Product Name | PPAR-beta/delta Antagonist II, GSK3787 |
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| Description | Purity ~99% (HPLC). A cell-permeable pyridylsulfone that acts as a selective, high affinity PPARb (PPARd) ligand (IC50 in PPAR ligand displacement assays =200nM against human PPARb and >10uM against PPARa or PPARg) and effectively antagonizes agonist-induced, but not basal, PPARb transcription activity both in cultures in vitro (IC50=126nM in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10mg/kg GW0742-induced Adr and Angptl4 mRNA upregulation, respectively, in colon epithelium; 10mg/kg GSK3787; p.o.) by covalently modifying PPARb at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARg (1.2-fold increase above basal level by 1uM GSK3787), and effectively block the more potent agonist GW1929 from further stimulation (1.5 and 3.5-fold above basal by 0.3uM GW1929 in the presence or absence of 1uM GSK3787, respectively). Formula: C15H12ClF3N2O3S Molecular Weight: 392.8 Solubility: DMSO (50mg/ml, clear, colorless solution) |
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| Size | 10mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | PPAR-beta/delta Antagonist II, GSK3787 (4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARb Antagonist I, PPARd Antagonist I) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217690 |
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| Order / More Info | PPAR-beta/delta Antagonist II, GSK3787 from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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