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首页-小分子抑制剂&激动剂-TGF-beta/Smad-TGF beta Receptor (TGFBR)-R-268712
R-268712

Chemical Structure : R-268712

CAS No.: 879487-87-3

R-268712 (R268712, R 268712)

货号: PC-43290Not For Human Use, Lab Use Only.

R-268712 is a potent, selective, orally active inhibitor of TGF-β type I receptor ALK5 with IC50 of 2.5 nM, >5,000-fold more selectivity than p38 MAPK.

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5 mg ¥980 In stock
10 mg ¥1480 In stock
25 mg ¥2580 In stock
50 mg ¥4280 In stock
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

R-268712 is a potent, selective, orally active inhibitor of TGF-β type I receptor ALK5 with IC50 of 2.5 nM, >5,000-fold more selectivity than p38 MAPK.
R-268712  inhibits the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model at doses of 1, 3 and 10mg/kg.
R-268712 also reduces proteinuria and glomerulosclerosis significantly with improvement of renal function in glomerulonephritis models.

物理化学性质&存储条件

分子量 363.3882
分子式 C20H18FN5O
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

1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-

参考文献

1. Terashima H, et al. Eur J Pharmacol. 2014 Jul 5;734:60-6

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