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J-1063
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
J-1063图片
CAS NO:2374772-46-8
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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]

ALK5

 

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

425.51

Formula

C24H19N5OS

CAS 号

2374772-46-8

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.