BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC 50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease In Vitro BMS-582949 displays a p38α IC 50 of 13 nM and a cellular TNFα IC 50 of 50 nM. BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model . Dosage: 1, 10, 100 mg/kg. Administration: Orally once daily (from day 11 to day 19). Result: Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg. Form:Solid IC50& Target:p38α MAPK 13 nM (IC 50 ) TNFα 50 nM (IC 50 , in cells)
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BMS-582949 hydrochloride
CAS number：912806-16-7 molecular formula：C22H27ClN6O2
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| Chinese alias | BMS-582949 盐酸盐 | ||
| English alias | 912806-16-7 (HCl) | UNII-3Z6GAP3R9Q | 4-[5-(Cyclopropylcarbamoyl)-2-methylanilino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide hydrochloride | BMS-582949 (hydrochloride) | BMS 582949 hydrochloride | AS-35330 | BMS 582949 HCL | 4-((5-(cycl | ||
| CAS number | 912806-16-7 | molecular formula | C22H27ClN6O2 |
| molecular weight | 442.94 g/mol | Exact mass | ≥98% |
| PSA | 100.000 Ų | logp | - |
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