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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-PPAR-GSK3787
GSK3787

Chemical Structure : GSK3787

CAS No.: 188591-46-0

GSK3787 (GSK 3787, GSK-3787)

货号: 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.

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25 mg ¥1380 In stock
50 mg ¥2280 In stock
100 mg ¥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 392.78
分子式 C15H12ClF3N2O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-chloro-N-(2-((5-(trifluoromethyl)pyridin-2-yl)sulfonyl)ethyl)benzamide

参考文献

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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