SB 525334

国际站：SB 525334

CAS：356559-20-1

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：SB 525334 是一种有效的选择性转化生长因子 β1 受体 (ALK5) 抑制剂，IC₅₀ 为 14.3 nM。 IC50 和目标：IC50：14.3 nM (ALK5)^[1] 体外： SB525334（1 μM；15 分钟后用 0.625 ng/ml TGF-β1，6 天后评估）抑制 TGF-β1 介导的家族性特发性肺动脉高压 (iPAH) 肺动脉平滑肌细胞 (PASMC) 增殖，IC₅₀ 为 295 nM^[2]。

体外：SB525334（1 μM；在用 0.625 ng/ml TGF-β1 刺激之前持续 15 分钟，6 天后评估）抑制 TGF-β1 介导的家族性特发性肺动脉高压 (iPAH) 肺动脉平滑肌细胞 (PASMC) 增殖IC₅₀ 为 295 nM ^[2]。

体内：SB525334（3-30 mg/kg；口服；从第 17 天到第 35 天每天）显着逆转肺动脉高压 (PAH) 大鼠模型中的肺动脉压^[2]。

参考文献：[1]. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.[2]. Thomas M, et al. ALK5 mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline.[3]. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899.