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Emprumapimod
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Emprumapimod图片
CAS NO:765914-60-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
PF-07265803
产品介绍
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

p38α

100 pM (IC50)

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

473.52

Formula

C24H29F2N5O3

CAS 号

765914-60-1

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.