R 268712, Potent and selective inhibitor of TGF-βRI, Each

Details

R 268712 is a potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ∽5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomerulosclerosis and improves renal function in an anti-Thy1 glomerulonephritis model. Orally bioavailable.