化合物 GW-6604 T9947

Product Introduction
Bioactivity


英文名: GW-6604

描述: 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。

体外活性: GW-6604在化学实验中抑制ALK5自磷酸化，IC50值为140 nM。在细胞实验中，GW-6604抑制TGF-beta诱导的PAI-1转录，IC50值为500 nM[2]。

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 2.98 mg/mL (10 mM)


关键字: GW-6604 | GW6604 | GW 6604

相关产品: TM5007 | Toddalolactone | Tiplaxtinin | TM5275 sodium | Aleplasinin | TM5441 | UK-371804 | AZ3976 | Upamostat | Loureirin B

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Metabolism Compound Library | TGF-beta/Smad Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途