| CAS NO: | 475085-57-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 475085-57-5 |
| 别名 | [4-[(5,6-二苯基吡嗪基)(1-甲基乙基)氨基]丁氧基]乙酸,ACT-333679 |
| Canonical SMILES | OC(COCCCCN(C(C)C)C1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)N=C1)=O |
| 分子式 | C25H29N3O3 |
| 分子量 | 419.52 |
| 溶解度 | DMSO : ≥ 50 mg/mL (119.18 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist. 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[1]. MRE-269 induces concentration-dependent vasodilation in LPA(+), LPA(-), and SPA(-)[3]. 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[1]. 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[2]. [1]. Fuchikami C, et al. A comparison of vasodilation mode among selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide]), its active metabolite MRE-269 and various prostacyclin receptor agonists in rat, porcin [2]. Orie NN, et al. Differential actions of the prostacyclin analogues treprostinil and iloprost and the selexipag metabolite, MRE-269 (ACT-333679) in rat small pulmonary arteries and veins. Prostaglandins Other Lipid Mediat. 2013 Oct;106:1-7 [3]. Kuwano K, et al. A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses |
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