R-268712 是一种口服有效的选择性 ALK-5 抑制剂，其 IC₅₀ 值为 2.5 nM。R-268712 能以剂量依赖的方式抑制 Smad3 的磷酸化，其 IC₅₀ 值为 10.4 nM。R-268712 通过抑制TGF-β 的信号传导来抑制肾小球肾炎以及肾小球硬化，可用于肾脏纤维化和癌症的研究。

R-268712 is an orally active and selective ALK-5 inhibitor, with an IC 50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC 50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.

Solid

TGFBR1 2.5 nM (IC50) Smad3 10.4 nM (IC

R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM in HFL-1 cells.R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC 0-24 values of 0.075, 0.28, 1.6 and 8.2 μg?h/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively.
R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model.
R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Terashima H, et al. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38.
[2]. Terashima H, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6.

In Vitro: DMSO : 125 mg/mL (343.98 mM; Need ultrasonic)配制储备液