ASK1-IN-2 (C09-1101-942)

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) , with an IC 50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitisIn VitroASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoASK1-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 (T 1/2 =1.45 h) in rats . ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUC last =4517 h•ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T 1/2 =2.31 h) in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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; T 1/2 =1.45 h. P.o.: AUC last =4517 h•ng/mL; F=62.2%; T 1/2 =2.31 h.Form:SolidIC50& Target:ASK1 32.8 nM (IC 50 ). Specification: 0.98 Molecular Formula: C19H17FN6O Molecular Weight: 364.38 PubChem CID: 155671000