MRE-269

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

熊果酸属于熊果烷三萜家族，其结构基于五环熊果烷骨架。它具有作为 HIV-1 蛋白酶抑制剂的潜力。

MRE-269, also known as ACT-333679, is a long-acting and highly selective prostacyclin receptor agonist. MRE-269, the active form or metabolite of Selexipag (NS-304), is much more selective for the IP receptor than are the prostacyclin analogs beraprost and iloprost, which also have high affinity for the EP(3) receptor.

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(-).

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.

MRE-269 | MRE269 | MRE 269 | ACT-333679

Others

Other Targets

HIV-1 protease

Cardiovascular Disease

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475085-57-5

419.52

C25H29N3O3

>98% (HPLC)

DMSO : ≥ 50 mg/mL. 119.18 mM; H2O : < 0.1 mg/mL

CC1CCC2(CCC3(C(=CCC4C3(CCC5C4(CCC(=O)C5(C)C)C)C)C2C1C)C)C(=O)O

2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid

(-20℃)

With Ice Pack

≥ 2 years