R-268712

ALK5抑制剂(IC50=2.5nM)；对ALK5具有选择性，优于p38MAPK(IC50=12µM)；以1、3和10mg/kg的剂量使用转基因Col1a1-LucTg大鼠，可降低单侧输尿管梗阻模型中的肾纤维化；以0.3和1mg/kg的剂量使用抗Thy-1肾小球肾炎模型，可降低半肾切除大鼠的蛋白尿和肾小球硬化，并改善肾功能。An inhibitor of ALK5 (IC50 = 2.5 nM); selective for ALK5 over p38 MAPK (IC50 = 12 µM); reduces renal fibrosis in a model of unilateral ureteral obstruction using transgenic Col1a1-Luc Tg rats at 1, 3, and 10 mg/kg; reduces proteinuria and glomerulosclerosis and improves renal function in heminephrectomized rats in a model of anti-Thy-1 glomerulonephritis at 0.3 and 1 mg/kg.分子式C20H18FN5O分子量363.4FC(C=C1)=C(C2=CN(CCO)N=C2)C=C1C3=CNN=C3C4=NC(C)=CC=C4