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Chemical Structure : GSK3787
CAS No.: 188591-46-0
Catalog No.: PC-20276Not For Human Use, Lab Use Only.
GSK3787 (GSK 3787) is a potent, selective and irreversible antagonist of PPARdelta (PPARδ) with binding pIC50 of 6.6, without measurable affinity for hPPARα or hPPARγ.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $188 | In stock | |
| 100 mg | $398 | In stock | |
| 250 mg | $588 | In stock | |
| 1 g | Get quote |
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GSK3787 (GSK 3787) is a potent, selective and irreversible antagonist of PPARdelta (PPARδ) with binding pIC50 of 6.6, without measurable affinity for hPPARα or hPPARγ.
GSK3787 shows equipotent species activity against the human and mouse receptor.
GSK3787 covalently modifies PPARδ Cys249 within the ligand binding pocket.
PPARδ antagonizes the induction of PPARδ-regulated target genes in skeletal muscle cells.
GSK3787 antagonizes GW0742-induced expression of Angptl4 in mouse fibroblasts, mouse keratinocytes, and human cancer cell lines.
| M.Wt | 392.78 | |
| Formula | C15H12ClF3N2O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-chloro-N-(2-((5-(trifluoromethyl)pyridin-2-yl)sulfonyl)ethyl)benzamide |
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1. Shearer BG, et al. J Med Chem. 2010 Feb 25;53(4):1857-61.
2. Palkar PS, et al. Mol Pharmacol. 2010 Sep;78(3):419-30.
3. Hack K, et al. PLoS One. 2012;7(5):e37097.
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