R-268712 是选择性的 ALK5 抑制剂(IC50:2.5 nM)。

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor.?Evaluation of in vitro inhibition indicated that R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK).

Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model.?Additionally, the efficacy of R-268712 in a heminephrectomized anti-Thy1 glomerulonephritis model at doses of 0.3 and 1mg/kg.?R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function.

879487-87-3

C20H18FN5O

363.39

DMSO:110 mg/mL (302.7 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years