J-1063 是一种有效的，具有选择性和口服活性的ALK5抑制剂，其IC50值为 0.039 μM. J-1063 通过抑制炎症浸润，胶原沉积，肝细胞坏死发挥抗肝纤维化作用。J-1063 具有研究肝纤维化的潜力。
| 生物活性 | J-1063 is a potent, selective and orally activeALK5inhibitor with anIC50of 0.039 μM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | J-1063 (compound 4) (10 mM) shows significant ALK5 inhibitory activity (IC50s of 8.12 and 0.039 μM for p38α MAP kinase and ALK5, respectively)[1].
J-1063 (2.5, 5, 10 μM; 1 h) improved fibroblast differentiation induced by TGF-β in LX-2 cells[1].
J-1063 (2.5, 5, 10 μM; 1 h) inhibits the inflammatory response induced by TGF-β[1].
J-1063 inhibits liver fibrosis by regulating TGF-β/Smad signaling and inhibits the activation of NLPR3-Caspase-1 inflammasome[1].
J-1063 (12.5 mg/kg; Cxcl1, Cxcl2 cells) inhibits the infiltration of macrophages and neutrophils during liver fibrosis[1].
Western Blot Analysis[1] | Cell Line: | LX-2 cells | | Concentration: | 2.5, 5, 10 μM | | Incubation Time: | 1 h | | Result: | Inhibited the inflammatory response induced by TGF-β. |
|
体内研究
(In Vivo) | J-1063 (12.5, 25, 50 mg/kg; i.g., one time per day for two weeks) shows no toxic side effects on mice at low dose and is suitable for therapeutic administration[1].
J-1063 (12.5 mg/kg; p.o., daily for two consecutive weeks) shows benefit for TAA-induced liver fibrosis in mice[1].
| Animal Model: | Male C57BL/6 mice[1] | | Dosage: | 12.5, 25, 50 mg/kg | | Administration: | i.g., one time per day, two weeks | | Result: | Showed no toxic side effects on mice at low dose and was suitable for therapeutic administration. |
| Animal Model: | Male C57BL/6 mice[1] | | Dosage: | 12.5 mg/kg | | Administration: | p.o., daily for two consecutive weeks | | Result: | Showed benefit for TAA-induced liver fibrosis in mice. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
