Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
性状
Solid
IC50 & Target[1][2]
p38α
体外研究(In Vitro)
Emprumapimod hydrochloride (ARRY-797) 抑制 RPMI-8226 细胞中 LPS 诱导产生的 IL-6,IC50 值为 100 pM。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Emprumapimod hydrochloride (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 hydrochloride (30 mg/kg;口服;一天两次持续 4 周) 防止 Lmna 小鼠左心室 (LV) 扩张和左心室缩短分数 (FS) 恶化。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Wright D, et al. ARRY-797, a potent and selective inhibitor of p38 map kinase, inhibits LPS-induced IL-6 and in vivo growth of RPMI-8226 human multiple myeloma cells[J]. 2006.[2]. Antoine Muchir, et al. Abnormal p38α mitogen-activated protein kinase signaling in dilated cardiomyopathy caused by lamin A/C gene mutation. Hum Mol Genet. 2012 Oct 1;21(19):4325-33.