| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S87213-5mg |
99.0% | ￥590.00 | 6 | - | - | - |
|
S87213-10mg |
99.0% | ￥990.00 | 6 | - | - | - |
|
S87213-25mg |
99.0% | ￥1590.00 | 6 | - | - | - |
|
S87213-50mg |
≥98% | ￥2530.00 | 货期：2-3天 | - | - | - |
|
S87213-100mg |
≥98% | ￥3970.00 | 货期：2-3天 | - | - | - |
|
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
| 产品描述： | 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 | ||||||||||||||||||||
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| 靶点： | p38α MAPK:13 nM (IC50);TNFα:50 nM (IC50, in cells);p38MAPK;Autophagy | ||||||||||||||||||||
| 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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| 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. | ||||||||||||||||||||
| 参考文献： | 1. Liu C, et al. Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. J Med Chem. 2010 Sep 23;53(18):6629-39. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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