Emprumapimod 是一种口服有效的、选择性p38α MAPK抑制剂，作用于RPMI-8226 细胞，直接抑制 LPS 诱导产生的 IL-6 (IC50=100 pM)。Emprumapimod 可用于扩张型心肌病和急性炎性疼痛的研究。
| 生物活性 | Emprumapimod is a potent, orally bioavailable and selective inhibitor ofp38αMAPKdirectly inhibits LPS-inducedIL-6production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain[1][2]. |
| IC50& Target | |
体内研究
(In Vivo) | In SCID-beige mice, LPS (3 μg/kg) induced IL-6 (7897±827 pg/mL) and TNF-α (1922±282 pg/mL) after 2 hours and these cytokines are inhibited by oral administration of Emprumapimod (ARRY-797; 30 mg/kg) by 91% and 95%, respectively[1].
In MM xenograft models, Emprumapimod (30 mg/kg, BID, PO) inhibits RPMI 8226 tumor growth by 72% as a single agent and by 56% when LPS is administered to stimulate growth in vivo[1].
Emprumapimod also inhibits LPS-induced phosphorylation of p38 in RPMI-8226 xenografts[1].
Treatment ofLmnaH222P/H222Pmice with the p38α inhibitor Emprumapimod (ARRY-371797; 30 mg/kg; orally twice daily; for 4 weeks initiated at 16 weeks of age) prevents left ventricular (LV) dilatation and deterioration of fractional shortening (FS). LV end-diastolic diameter (LVEDD) and LV end-systolic diameter (LVESD) inLmnaH222P/H222Pmice treated with Emprumapimod are significantly smaller and FS is significantly increased compared with the placebo-treated mice[2].
| Animal Model: | LmnaH222P/H222Pmice were[2] | | 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. |
|
| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com