耗材描述
MRE-269
产品活性:MRE-269 是 selexipag 的有效代谢物,同时为选择性的 IP 受体激动剂。
产品来源: https://www.medchemexpress.cn/MRE-269.html
研究领域:GPCR/G Protein
作用靶点:Prostaglandin Receptor
结构分类:酮、醛、酸 | 结构分类
In Vitro: 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: 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.
相关产品:Natural Product Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Natural Product Library | Anti-Cardiovascular Disease Compound Library | Endocrinology Compound Library | Angiogenesis-Related Compound Library | Human Metabolite Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | Bioactive Compound Library Max | Prostaglandin E2 | EIPA | Prostaglandin E1 | Tranilast | U-46619 | PF-04418948 | Prostaglandin D2 | Dinoprost | Latanoprost | ONO-AE3-208 | Iloprost | Palupiprant | Selexipag | Treprostinil | L-798106 | Grapiprant | 16,16-Dimethyl prostaglandin E2 | DG-041 | Fevipiprant | GW627368 | Laropiprant | Asapiprant | L-161982 | AH 6809 | Ramatroban | RO1138452 | Cefminox sodium | Travoprost | Bimatoprost
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