BMS-582949

A p38α MAP kinase inhibitor

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货号: ajci18236
CAS: 623152-17-0
别名:
分子式: C22H26N6O2
分子量: 406.48
纯度: >98%
溶解度: DMF: 30 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 15 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): slightly soluble
储存: Store at -20°C
库存: 现货

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.