VX-702
货号：
13108-5mg 基本售价：
266.0 元 规格：
5 mg
产品信息
概述| 货号 | 13108-5mg |
| 描述 | VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion.1 It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.1 VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.2 Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.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).
2.Kuliopulos, A.,Mohanlal, R. and Covic, L. Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation. Thrombosis and Haemostasis 92, 1387-1393 (2004).
3.Damjanov, N.,Kauffman, R.S. and Spencer-Green, G.T. Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: Results of two randomized, double-blind, placebo-controlled clinical studies. Arthritis and Rheumatism 60(5), 1232-1241 (2009).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 404.3 |
| 分子式 | C19H12F4N4O2 |
| CAS号 | 745833-23-2 |
| 稳定性 | ≥ 2 years |
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