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BMS-582949
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-582949图片
CAS NO:623152-17-0
规格:98%
分子量:406.48
包装与价格:
包装价格(元)
1mg电议
5mg电议
25mg电议

产品介绍
p38 MAPK inhibitor
CAS:623152-17-0
分子式:C22H26N6O2
分子量:406.48
纯度:98%
存储:Store at -20°C

Background:

IC50: 13 nM


BMS-582949 is a p38 MAPK inhibitor


p38R MAP kinase plays a key role in regulating the biosynthesis of various inflammatory cytokines, such as tumor necrosis factor alpha and interleukin-1β. Thus, p38R inhibitors are considered as a promising therapy for inflammatory disease treatment.


In vitro: BMS-582949 was found to be 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective against Raf. Moreover, the binding mode of BMS-582949 with p38R was further demonstrated by X-ray crystallographic analyses [1].


In vivo: In a pseudoestablished rat adjuvant arthritis model, BMS-582949 at doses of 10 and 100 mg/kg was found to display dose-dependent reduction in paw swelling with qd dosing. In addition, with bid dosing at doses of 1 and 5 mg/kg, BMS-582949 showed improved efficacy, resulting in great reduction in paw swelling. Moreover, the statistically significant reduction in paw swelling was also observed with the treatment of BMS-582949 at doses as low as 0.3 mg/kg bid [1].


Clinical trial: A multicenter FDG-PET trial showed that in stable atherosclerosis, 12 weeks of treatment with BMS-582949 was not able to reduce arterial inflammation or hs-CRP when compared with placebo, while intensification of statin therapy could decrease arterial inflammation significantly [2].


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.
[2]. Emami H, et al. The effect of BMS-582949, a P38 mitogen-activated protein kinase (P38 MAPK) inhibitor on arterial inflammation: a multicenter FDG-PET trial. Atherosclerosis. 2015 Jun;240(2):490-6.