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编 号：F408659
分子式：C22H26N6O2
分子量：406.48
分子式：C22H26N6O2
分子量：406.48
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CAS No: 623152-17-0
产品详情
生物活性：
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis.
体内研究：
BMS-582949 (5 mg/kg， p.o.， 90 min) 显著降低 LPS 诱导的 BALB/c 雌性急性炎症小鼠模型中 TNFα 的产生。BMS-582949 (0.3-100 mg/kg， p.o.， q.d/b.i.d) 显著减少爪肿胀。BMS-582949 静脉注射 (i.v.) 的溶解方案使用 25% 的 N-甲基吡咯烷酮，33% 的聚乙二醇 400，9% 的丙二醇和 33% 的水作为溶剂。BMS-582949 口服灌胃 (p.o.) 溶解方案使用聚乙二醇 400 作为溶剂。Animal Model:murine models of acute inflammation from BALB/c female mice
Dosage:5 mg/kg
Administration:Oral gavage (p.o.), detection content at 90 min after LPS injection
Result:Reduced the TNFα production by 89% at 2 h, by 78% at 6 h before the LPS challenge.
Animal Model:Rat adjuvant arthritis (rat AA) models from Male Lewis rats
Dosage:1, 10, 100 mg/kg, once daily (q.d)
Administration:Oral gavage (p.o.)
Result:Reduced paw swelling with dose-dependent, with efficacy observed at doses of 10 and 100 mg/kg.
Animal Model:Rat adjuvant arthritis (rat AA) models from Male Lewis rats
Dosage:0-5 mg/kg, b.i.d
Administration:Oral gavage (p.o.)
Result:Improved efficacy markedly of reduction in paw swelling at doses of 1 and 5 mg/kg.Reduced paw swelling significantly at doses as low as 0.3 mg/kg.
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis.
体内研究：
BMS-582949 (5 mg/kg， p.o.， 90 min) 显著降低 LPS 诱导的 BALB/c 雌性急性炎症小鼠模型中 TNFα 的产生。BMS-582949 (0.3-100 mg/kg， p.o.， q.d/b.i.d) 显著减少爪肿胀。BMS-582949 静脉注射 (i.v.) 的溶解方案使用 25% 的 N-甲基吡咯烷酮，33% 的聚乙二醇 400，9% 的丙二醇和 33% 的水作为溶剂。BMS-582949 口服灌胃 (p.o.) 溶解方案使用聚乙二醇 400 作为溶剂。Animal Model:murine models of acute inflammation from BALB/c female mice
Dosage:5 mg/kg
Administration:Oral gavage (p.o.), detection content at 90 min after LPS injection
Result:Reduced the TNFα production by 89% at 2 h, by 78% at 6 h before the LPS challenge.
Animal Model:Rat adjuvant arthritis (rat AA) models from Male Lewis rats
Dosage:1, 10, 100 mg/kg, once daily (q.d)
Administration:Oral gavage (p.o.)
Result:Reduced paw swelling with dose-dependent, with efficacy observed at doses of 10 and 100 mg/kg.
Animal Model:Rat adjuvant arthritis (rat AA) models from Male Lewis rats
Dosage:0-5 mg/kg, b.i.d
Administration:Oral gavage (p.o.)
Result:Improved efficacy markedly of reduction in paw swelling at doses of 1 and 5 mg/kg.Reduced paw swelling significantly at doses as low as 0.3 mg/kg.
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