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首页-小分子抑制剂&激动剂-GPCR-Free Fatty Acid Receptor (FFAR)-AZ13581837
AZ13581837

Chemical Structure : AZ13581837

CAS No.: 2896777-27-6

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AZ13581837 (AZ 13581837)

货号: PC-20425Not For Human Use, Lab Use Only.

AZ13581837 is a potent, selective GPR120 (FFAR4) agonist with EC50 of 5.2 nM and 4.3 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

    AZ13581837 is a potent, selective GPR120 (FFAR4) agonist with EC50 of 5.2 nM and 4.3 nM for stimulation of DMR response in CHO-hGPR120/mGPR120 cells, respectively.
    AZ13581837 has IC50 of 120 nM calcium mobilization assays, does not activate mouse GPR40 in a calcium mobilization assay.
    AZ13581837 is about 100-fold more potent than Metabolex-36, AZ13581837 is selective for human and mouse GPR120 without activity on GPR40.
    AZ13581837 selectively induces a calcium response in CHO-hGPR120 cells with EC50 of 120 nM, induces GPR120 dependent calcium mobilization, DMR response and cAMP production in GPR120 overexpressing cells.
    AZ13581837 (10 uM) inhibits cAMP production in mouse islets and increase GLP-1 secretion from STC-1 cells.
    AZ13581837 (18 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 362.40
    分子式 C20H14N2O3S
    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

    2-(3-ethynyl-5-(3-pyridyloxy)phenyl)-3H-1,2-benzothiazole 1,1-dioxide

    参考文献

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

    2. Marine L Croze, et al. Mol Metab. 2021 Mar;45:101166.

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