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首页-小分子抑制剂&激动剂-GPCR-Adrenergic Receptor-MK-4618
MK-4618

Chemical Structure : MK-4618

CAS No.: 1190389-15-1

MK-4618 (MK 4618;MK4618;Vibegron;KRP-114V;RVT-901)

货号: PC-60734Not For Human Use, Lab Use Only.

MK-4618 (Vibegron, KRP-114V, RVT-901) is a potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    MK-4618 (Vibegron, KRP-114V, RVT-901) is a potent and selective full β3 adrenergic receptor agonist with EC50 of 1.1 nM.
    MK-4618 (Vibegron) displays no activity for β1 and β2 receptors (EC50>20 uM).
    MK-4618 (Vibegron) dose-dependently increases bladder capacity, decreased micturition pressure, and increased bladder compliance in rhesus monkeys, dose-dependently increases the circulating glycerol and fatty acid levels in rhesus and rat in vivo.
    MK-4618 (Vibegron) shows the potential for treatment of overactive bladder with M2/M3 antimuscarinics.

    物理化学性质&存储条件

    分子量 444.535
    分子式 C26H28N4O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-N-(4-(((2S,5R)-5-((R)-hydroxy(phenyl)methyl)pyrrolidin-2-yl)methyl)phenyl)-4-oxo-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrimidine-6-carboxamide

    参考文献

    1. Edmondson SD, et al. J Med Chem. 2016 Jan 28;59(2):609-23.

    2. Di Salvo J, et al. J Pharmacol Exp Ther. 2017 Feb;360(2):346-355.

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