Emprumapimod hydrochloride_product_DataBase

Bioactivity	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[1][2].
Invitro	Emprumapimod hydrochloride (ARRY-797) 抑制 RPMI-8226 细胞中 LPS 诱导产生的 IL-6，IC50 值为 100 pM[1]。
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%)[1]。Emprumapimod hydrochloride (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[2]。
Name	Emprumapimod hydrochloride
Formula	C24H30ClF2N5O3
Molar Mass	509.98
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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.

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