MRE-269

MRE-269CAS号: 475085-57-5分子式: C25H29N3O3分子量: 419.52描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
ACT-333679
外观
Off-White to Light Yellow Solid
可溶性/溶解性
DMSO : 50 mg/mL (119.18 mM; Need ultrasonic)
生物活性
靶点
Prostaglandin Receptor
In vitro(体外研究)
MRE-269 induces endothelium-independent vasodilation of rat extralobar pulmonary artery (EPA). MRE-269 or other IP receptor agonists including epoprostenol, iloprost, treprostinil and beraprost increase cAMP levels in hPASMC. MRE-269 induces concentration-dependent vasodilation in LPA(+), LPA(-), and SPA(-).
In vivo(体内研究)
The vasorelaxant effects of MRE-269 on rat small intralobar pulmonary artery (SIPA) and EPA are the same, while the other IP receptor agonists induce less vasodilation in SIPA than in EPA. MRE-269 produces substantial relaxation of rat small pulmonary artery, although its effects are only significant at high concentrations of above 10 μM (pEC50, 4.98±0.22). By contrast, in rat small pulmonary veins, MRE-269 only produces minimal relaxation over the whole concentration range, with only significant relaxation occurring at the two highest doses of MRE-269 of 10 and 100 μM.

分子结构图

MRE-269