J-1063,2374772-46-8

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J-1063

CAS No. : 2374772-46-8

MCE 国际站：J-1063

产品活性：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。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

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).
J-1063 (2.5, 5, 10 µM; 1 h) improved fibroblast differentiation induced by TGF-β in LX-2 cells.
J-1063 (2.5, 5, 10 µM; 1 h) inhibits the inflammatory response induced by TGF-β.
J-1063 inhibits liver fibrosis by regulating TGF-β/Smad signaling and inhibits the activation of NLPR3-Caspase-1 inflammasome.
J-1063 (12.5 mg/kg; Cxcl1, Cxcl2 cells) inhibits the infiltration of macrophages and neutrophils during liver fibrosis.

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.
J-1063 (12.5 mg/kg; p.o., daily for two consecutive weeks) shows benefit for TAA-induced liver fibrosis in mice.

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