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BMS-582949 hydrochloride

CAS No. : 912806-16-7

MCE 国际站：BMS-582949 hydrochloride

产品活性：BMS-582949 hydrochloride 是具有口服活性的、高度选择性的p38α MAPK 抑制剂，其IC₅₀ 值为13 nM。BMS-582949 hydrochloride 具有明显改善的药代动力学特征，能用于炎症性疾病的研究。

研究领域：MAPK/ERK Pathway  |  Autophagy

作用靶点：p38 MAPK  |  Autophagy

In Vitro: BMS-582949 displays a p38α IC₅₀ of 13 nM and a cellular TNFα IC₅₀ 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.

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.

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