GW-6604 是一种 ALK5 抑制剂，具有明显的抗纤维化作用，可改善肝功能。

GW-6604 is an ALK5 inhibitor and shows clear antifibrotic effects resulting in liver function improvement.

GW-6604 inhibited autophosphorylation of ALK5 with an IC50 of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC50 = 500 nM)[2].

GW-6604 (40 mg/kg p.o.) increased liver regeneration in TGF-beta-overexpressing mice, which had undergone partial hepatectomy. In an acute model of liver disease, GW-6604 reduced by 80% the expression of collagen IA1. In a chronic model of DMN-induced fibrosis where DMN was administered for 6 weeks and GW-6604 dosed for the last 3 weeks (80 mg/kg p.o., b.i.d.), mortality was prevented and DMN-induced elevations of mRNA encoding for collagen IA1, IA2, III, TIMP-1 and TGF-beta were reduced by 50-75%. Inhibition of matrix genes overexpression was accompanied by reduced matrix deposition and reduction in liver function deterioration, as assessed by bilirubin and liver enzyme levels[2].

452342-37-9

C19H14N4

298.34

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years