您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > MRE-269(ACT-333679)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MRE-269(ACT-333679)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRE-269(ACT-333679)图片
CAS NO:475085-57-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
MRE-269 (ACT-333679) 是 selexipag 的活性代谢物,可作为选择性 IP 受体激动剂。
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 SMILESOC(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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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