CAS:879487-87-3R268712

R268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

879487-87-3

储存条件

分子式

C20H18FN5O

运输

蓝冰

分子量

363.39

别名

溶解度

DMSO	120.0 mg/mL (330.2 mM) warming

动物实验配方

生物活性

描述The transforming growth factor β (TGF-β) is a key regulator of renal fibrosis that stimulates epithelial to mesenchymal transition and the production of extracellular matrix proteins. The activin receptor-like kinase 5 (ALK5) is a TGF-β type I receptor responsible for the phosphorylation of Smad 2/3 proteins. R268712 is a potent and selective ALK5 inhibitor with an IC50 value of 2.5 nM, but shows a weak inhibitory effect on p38 MAP kinase (IC50 = 12.1 μM). The administration of R268712 (1–10 mg/kg) in a mouse model of unilateral ureter obstruction inhibited renal luciferase activity in a dose-dependent manner. R268712 at a dosage of 1 mg/kg also significantly reduced proteinuria at day 21 post-treatment. In a heminephrectomized anti-Thy1 glomerulonephritis model, mice treated with R268712 at a concentration of 10 mg/kg showed suppressed weight gain compared with the control group^[2].
作用机制R268712 is a potent inhibitor of ALK5 that exhibits antifibrotic activity in a mouse model of unilateral ureter obstruction and a mouse model of anti-Thy1 glomerulonephritis^[2].