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编 号:F760205
分子式:C24H29F2N5O3
分子量:473.52
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1mg
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5mg
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生物活性:
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.

体内研究:
Emprumapimod (ARRY-797) (30 mg/kg;口服) 在 SCID-beige 小鼠中抑制 IL-6 (91%) 和 TNF-α (95%) 的表达,在 RPMI-8226 异种移植物中抑制 p38 的磷酸化,在多发性骨髓瘤 (MM) 异种移植模型中抑制 RPMI-8226 肿瘤的生长 (72%)。Emprumapimod (30 mg/kg;口服;一天两次持续 4 周) 防止 LmnaH222P/H222P 小鼠左心室 (LV) 扩张和左心室缩短分数 (FS) 恶化。Animal Model:LmnaH222P/H222P mice were
Dosage:30 mg/kg
Administration:Administered orally by gavage starting when mice were 16 weeks of age and continuing until 20 weeks of age
Result:There were significant increases in LVEDD and LVESD as well as a decrease in FS, a parameter directly proportional to the LV ejection fraction.

体外研究:
Emprumapimod (ARRY-797) 抑制 LPS 诱导的 RPMI-8226 细胞产生 IL-6,IC50 值为 100 pM。
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