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编 号：F751630
分子式：C24H19N5OS
分子量：425.51
分子式：C24H19N5OS
分子量：425.51
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CAS No: 2374772-46-8
产品详情
生物活性：
J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 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.
体内研究：
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.Animal Model:Male C57BL/6 mice
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
Dosage:12.5 mg/kg
Administration:p.o., daily for two consecutive weeks
Result:Showed benefit for TAA-induced liver fibrosis in mice.
体外研究：
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.
J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 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.
体内研究：
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.Animal Model:Male C57BL/6 mice
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
Dosage:12.5 mg/kg
Administration:p.o., daily for two consecutive weeks
Result:Showed benefit for TAA-induced liver fibrosis in mice.
体外研究：
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.
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