Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5nM). 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.
Chemical Name: 4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
CAS Number: 879487-87-3
Solubility: Soluble to 100mM in DMSO and to 50mM in ethanol
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