| Identification | Back Directory | [Name]
1H-Pyrazole-1-acetamide, 3-(6-methyl-2-pyridinyl)-N-phenyl-4-thieno[3,2-c]pyridin-2-yl- | [CAS]
2374772-46-8 | [Synonyms]
J-1063
1H-Pyrazole-1-acetamide, 3-(6-methyl-2-pyridinyl)-N-phenyl-4-thieno[3,2-c]pyridin-2-yl- | [Molecular Formula]
C24H19N5OS | [MOL File]
2374772-46-8.mol | [Molecular Weight]
425.51 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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. |
| [IC 50]
ALK5 | [References]
[1] Zheng GH, et al. The in vitro and in vivo study of a pyrazole derivative, J-1063, as a novel anti-liver fibrosis agent: Synthesis, biological evaluation, and mechanistic analysis. Bioorg Chem. 2022; 122:105715. DOI:10.1016/j.bioorg.2022.105715 |
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