产品信息
抗原名称
EP4
商品描述
MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed strong binding affinity for the EP4 receptor with Ki of 0.7 nM,
分子量
603.69
纯度
98%
可溶性
DMSO: ≥ 31 mg/mL
外观
Light yellow to yellow Solid
In vitro(体外研究)
MF498 was a selective EP4 receptor antagonist with the Ki of 0.7 nM while the Ki > 1 μM for other EP receptors. In HEK293 cells expressing human EP4 receptor, MF498 inhibited EP ligand-induced activity with an IC50 value of 1.7 nM.
In vivo(体内研究)
In rodent models of rheumatoid and osteoarthritis, MF498 inhibited inflammation without gastrointestinal toxicity, the ED50 values was as low as 0.02 mg/kg/day.In adjuvant-induced arthritis (AIA) rat model for rheumatoid arthritis (RA), MF498 inhibited inflammation. In addition, MF498 was effective in relieving OA-like pain in guinea pigs. In rat models of gastrointestinal toxicity, MF498 was well tolerated, causing no mucosal leakage or erosions. In a furosemide-induced diuresis model, MF498 reduced furosemide-induced natriuresis by 50% .
背景
别名
MF-498； MF 498
分子式
C32H33N3O7S
CAS号
915191-42-3
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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