| Bioactivity | 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[1][2]. |
| Invitro | Emprumapimod (ARRY-797) 抑制 LPS 诱导的 RPMI-8226 细胞产生 IL-6，IC50 值为 100 pM[1]。 |
| In Vivo | 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%)[1]。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[2]。 Animal Model: |
| Name | Emprumapimod |
| CAS | 765914-60-1 |
| Formula | C24H29F2N5O3 |
| Molar Mass | 473.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Dale Wright, 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. [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. |