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首页-小分子抑制剂&激动剂-GPCR-Free Fatty Acid Receptor (FFAR)-Metabolex-36
Metabolex-36

Chemical Structure : Metabolex-36

CAS No.: 1224102-57-1

Metabolex-36 (Metabolex 36)

货号: PC-20424Not For Human Use, Lab Use Only.

Metabolex-36 is a potent, selective GPR120 (FFAR4) agonist with EC50 of 570 nM and 130 nM for stimulation of DMR response in CHO-hGPR120/mGPR120 cells, respectively.

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

    生物&药学活性

    Metabolex-36 is a potent, selective GPR120 (FFAR4) agonist with EC50 of 570 nM and 130 nM for stimulation of DMR response in CHO-hGPR120/mGPR120 cells, respectively.
    Metabolex-36 has IC50 of 1.3 uM calcium mobilization assays, does not activate mouse GPR40 in a calcium mobilization assay.
    Metabolex-36 is selective for human and mouse GPR120 without activity on GPR40.
    Metabolex-36 induces GPR120 dependent calcium mobilization, DMR response and cAMP production in GPR120 overexpressing cells.
    Metabolex-36 (10 uM) inhibits cAMP production in mouse islets and increase GLP-1 secretion from STC-1 cells.
    Metabolex-36 (30 mg/kg) improve oral glucose tolerance, increases insulin secretion in IVGTT in lean mice.

    物理化学性质&存储条件

    分子量 420.84
    分子式 C21H19ClF2N2O3
    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

    (R)-3-(4-((1-(4-chlorophenyl)-3-methyl-1H-pyrazol-5-yl)methoxy)-3,5-difluorophenyl)-2-methylpropanoic acid

    参考文献

    1. Sundström L, et al. PLoS One. 2017 Dec 5;12(12):e0189060.

    2. Ma J, et al. Aryl GPR120 receptor agonist and uses thereof. International patent WO 2020/048207. 2010.

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