| CAS NO: | 623152-17-0 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| Cas No. | 623152-17-0 |
| 化学名 | 4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide |
| Canonical SMILES | O=C(C1=CN2N=CN=C(NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C)NCCC |
| 分子式 | C22H26N6O2 |
| 分子量 | 406.48 |
| 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 |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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]. References: |
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