| Bioactivity | GW-6604 is an ALK5 inhibitor with an IC50 value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis[1]. |
| Invitro | GW-6604(0-10 μM, )抑制 HepG2 细胞中 TGF-β 诱导的 PAI-1 转录和分泌的 IC50 值为 500 nM，有效阻断了 Smad 依赖性反应[1]。 |
| In Vivo | GW-6604(p.o., 25-80 mg/kg, twice a day, 3 weeks)在 SD 大鼠急性 DMN 模型中，依赖性地抑制肝脏 COL IA1 过度表达，使其表达降低了 80%。保持了正常的肝脏重量，有效减少了肝纤维化以及增加基质退化[1]。 |
| Name | GW-6604 |
| CAS | 452342-37-9 |
| Formula | C19H14N4 |
| Molar Mass | 298.34 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Anne-Charlotte de Gouville, et al. Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol. 2005 May;145(2):166-77. |