产品
编 号：F516971
分子式：C22H27ClN6O2
分子量：442.94
分子式：C22H27ClN6O2
分子量：442.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 912806-16-7
产品详情
生物活性：
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
体内研究：
BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency.Animal Model:Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model.
Dosage:1, 10, 100 mg/kg.
Administration:Orally once daily (from day 11 to day 19).
Result:Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.
体外研究：
BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM.BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms.
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
体内研究：
BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency.Animal Model:Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model.
Dosage:1, 10, 100 mg/kg.
Administration:Orally once daily (from day 11 to day 19).
Result:Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.
体外研究：
BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM.BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms.
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