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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-PPAR-GSK0660
GSK0660

Chemical Structure : GSK0660

CAS No.: 1014691-61-2

GSK0660 (GSK-0660;GSK 0660)

货号: PC-43009Not For Human Use, Lab Use Only.

GSK0660 is a potent, selective, dual PPARβ/δ antagonist with pIC50 of 6.8 (160 nM), shows no activity on PPARα and PPARγ (IC50>10 uM).

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10 mg ¥1180 In stock
25 mg ¥2180 In stock
50 mg ¥3580 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

GSK0660 is a potent, selective, dual PPARβ/δ antagonist with pIC50 of 6.8 (160 nM), shows no activity on PPARα and PPARγ (IC50>10 uM).
GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.53, reduces CPT1a expression in skeletal muscle cells with EC50 of 100 nM, as well as ANGPTL4 but not PDK4.
GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells.

物理化学性质&存储条件

分子量 418.4866
分子式 C19H18N2O5S2
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

DMSO: ≥ 49 mg/mL

Chemical Name/SMILES

2-Thiophenecarboxylic acid, 3-[[[2-methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-, methyl ester

参考文献

1. Shearer BG, et al. Mol Endocrinol. 2008 Feb;22(2):523-9.

2. Jiménez R, et al. J Pharmacol Exp Ther. 2010 Feb;332(2):554-61.

3. Riahi Y, et al. Diabetes. 2010 Apr;59(4):808-18.

4. Lee WJ, et al. J Cell Biochem. 2018 Feb 1. doi: 10.1002/jcb.26732.

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