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Firuglipel

Chemical Structure : Firuglipel

CAS No.: 1371591-51-3

Firuglipel (DS-8500;DS8500a)

Catalog No.: PC-60042Not For Human Use, Lab Use Only.

Firuglipel (DS-8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells, displays no significant effect on 66 receptors, channels, or transporters.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    Firuglipel (DS-8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells, displays no significant effect on 66 receptors, channels, or transporters; enhances glucose-stimulated insulin secretion in Sprague-Dawley rats and promotes GLP-1 secretion in Zucker fatty rats, preserved β cell function and prevented increases in glycohemoglobin concentrations in rodent models of type 2 diabetes.

    Diabetes

    Phase 2 Clinical

    Physicochemical Properties

    M.Wt 467.497
    Formula C25H26FN3O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-(5-{(1R)-1-[4-(cyclopropanecarbonyl)phenoxy]propyl}-1,2,4-oxadiazol-3-yl)-2-fluoro-N-[(2R)-1-hydroxypropan-2-yl]benzamide

    References

    1. Patent WO2012050151.

    2. Inagaki N, et al. BMJ Open Diabetes Res Care. 2017 Sep 29;5(1):e000424.

    3. Terauchi Y, et al. J Diabetes Investig. 2018 Apr 1. doi: 10.1111/jdi.12846.

    4. Makino C, et al. Xenobiotica. 2018 Aug 20:1-33. doi: 10.1080/00498254.2018.1514545.

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