VX-745
货号：
18075-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 18075-1mg |
| 描述 | p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.1 It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.1 VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Duffy, J.P.,Harrington, E.M.,Salituro, F.G., et al. The discovery of VX-745: A novel and selective P38α kinase inhibitor. ACS Med.Chem.Lett. 2, 758-763 (2011).
2.Goldstein, D.M.,Kuglstatter, A.,Lou, Y., et al. Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. Journal of Medicinal Chemistry 53, 2345-2353 (2010).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 436.3 |
| 分子式 | C19H9Cl2F2N3OS |
| CAS号 | 209410-46-8 |
| 稳定性 | ≥ 2 years |
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