产品
编 号：F741648
分子式：C19H17FN6O
分子量：364.38
分子式：C19H17FN6O
分子量：364.38
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
询价
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25mg
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询价
50mg
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询价
结构图
CAS No: 2541792-70-3
产品详情
生物活性：
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.
体内研究：
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice.ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues.ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats.ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h?ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats.Animal Model:Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water
Dosage:25 mg/kg
Administration:P.o. daily for 7 days
Result:Induced a significant recovery of body weight loss, with an increase of +11.2%.Decreased the disease activity index (DAI) score about a 2 unit.Significantly prevented colon shortening.Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.
Animal Model:Male SD rats
Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:I.v. and p.o. administration
Result:I.v.: CL=1.38 L/h/kg; T1/2=1.45 h.P.o.: AUClast=4517 h?ng/mL; F=62.2%; T1/2=2.31 h.
体外研究：
ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%.
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.
体内研究：
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice.ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues.ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats.ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h?ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats.Animal Model:Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water
Dosage:25 mg/kg
Administration:P.o. daily for 7 days
Result:Induced a significant recovery of body weight loss, with an increase of +11.2%.Decreased the disease activity index (DAI) score about a 2 unit.Significantly prevented colon shortening.Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.
Animal Model:Male SD rats
Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:I.v. and p.o. administration
Result:I.v.: CL=1.38 L/h/kg; T1/2=1.45 h.P.o.: AUClast=4517 h?ng/mL; F=62.2%; T1/2=2.31 h.
体外研究：
ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%.
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