| Bioactivity | BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis[1]. |
| In Vivo | BMS-582949 (5 mg/kg， p.o.， 90 min) 显著降低 LPS 诱导的 BALB/c 雌性急性炎症小鼠模型中 TNFα 的产生[1]。BMS-582949 (0.3-100 mg/kg， p.o.， q.d/b.i.d) 显著减少爪肿胀[1]。BMS-582949 静脉注射 (i.v.) 的溶解方案使用 25% 的 N-甲基吡咯烷酮，33% 的聚乙二醇 400，9% 的丙二醇和 33% 的水作为溶剂[1]。BMS-582949 口服灌胃 (p.o.) 溶解方案使用聚乙二醇 400 作为溶剂[1]。 Animal Model: |
| Name | BMS-582949 |
| CAS | 623152-17-0 |
| Formula | C22H26N6O2 |
| Molar Mass | 406.48 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |