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首页-小分子抑制剂&激动剂-GPCR-Free Fatty Acid Receptor (FFAR)-CPL207280
CPL207280

Chemical Structure : CPL207280

CAS No.: 2361497-72-3

CPL207280 (CPL 207280)

货号: PC-72119Not For Human Use, Lab Use Only.

CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).

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

    生物&药学活性

    CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).
    CPL207280 did not demonstrate any activity on the related GPR receptors, i.e., GPR41 (FFA2), GPR43 (FFA3), GPR55, GPR119, GPR120, GPR142, PPARα, or PPARγ at 10 uM.
    At 10 uM, CPL207280 showed 3.9 times greater enhancement of glucose-stimulated insulin secretion in mouse MIN6 pancreatic β-cells.
    CPL207280 improved glucose tolerance and increased insulin area in diabetic rats. CPL207280 is a potent enhancer of glucose-stimulated insulin secretion in animal disease models with no risk of hypoglycemia at therapeutic doses.

    物理化学性质&存储条件

    分子量 286.371
    分子式 C18H22O3
    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)-3-(4-((2,3-dimethylbut-2-en-1-yl)oxy)phenyl)hex-4-ynoic acid

    参考文献

    1. Bazydlo-Guzenda K, et al. Mol Pharmacol. 2021 Oct;100(4):335-347.

    2. Smuga D, et al. Eur J Med Chem. 2021 Dec 15;226:113810.

    3. Bazydlo-Guzenda K, et al. PLoS One. 2021 Sep 23;16(9):e0257477.

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