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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-KMN-159
KMN-159

Chemical Structure : KMN-159

CAS No.: 1544280-82-1

KMN-159 (KMN159)

货号: PC-49034Not For Human Use, Lab Use Only.

KMN-159 is a potent, selective small-molecule full agonist of the prostaglandin E2 type 4 (EP4) receptor with Ki of 0.24 nM (rEP4) and EC50 of 10.6 nM in the BMC ALP assays, with no affinity for EP2 (Ki>10,000 nM).

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

    生物&药学活性

    KMN-159 is a potent, selective small-molecule full agonist of the prostaglandin E2 type 4 (EP4) receptor with Ki of 0.24 nM (rEP4) and EC50 of 10.6 nM in the BMC ALP assays, with no affinity for EP2 (Ki>10,000 nM).
    KMN-159 demonstrates the ability to stimulate osteoblastic differentiation in vitro in total rat bone marrow from both sexes and from young and old rats as measured by induction of ALP enzyme activity, mineralized nodule formation, and osteoblast phenotype marker gene expression.
    KMN-159 can increase the rate of defect closure significantly over vehicle to that equivalent to rhBMP-2 in a rat calvarial defect model.

    物理化学性质&存储条件

    分子量 399.479
    分子式 C21H31F2NO4
    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

    7-((R)-3,3-difluoro-5-((3S,4S,E)-3-hydroxy-4-methylnon-1-en-6-yn-1-yl)-2-oxopyrrolidin-1-yl)heptanoic acid

    参考文献

    1. Barrett SD, et al. J Med Chem. 2019 May 9;62(9):4731-4741.

    2. Owen TA, et al. Gene. 2020 Jul 20;748:144668.

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