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Emprumapimod

CAS No. : 765914-60-1

MCE 站：Emprumapimod

产品活性：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。

研究领域：MAPK/ERK Pathway

作用靶点：p38 MAPK

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.
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. Emprumapimod also inhibits LPS-induced phosphorylation of p38 in RPMI-8226 xenografts.
Treatment of Lmna^H222P/H222P mice 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) in Lmna^H222P/H222P mice treated with Emprumapimod are significantly smaller ａnd FS is significantly increased compared with the placebo-treated mice.

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