ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice[1].
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[1].
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[1].
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 hng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1].
| Animal Model: | Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water[1] |
| 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 [1] |
| 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 hng/mL; F=62.2%; T1/2=2.31 h.
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