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GSK3395879

Chemical Structure : GSK3395879

CAS No.: 2215852-91-6

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GSK3395879 (GSK-3395879;GSK 3395879)

Catalog No.: PC-35713Not For Human Use, Lab Use Only.

GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4).

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

    Biological Activity

    GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4).
    GSK3395879 exhibits little or no activity against a broad panel of TRP channels (IC50 > 10µM for TRPA1, TRPV1, TRPM2, TRPM4, TRPM8, TRPC3, TRPC4, TRPC5, TRPC6).
    GSK3395879 demonstrates the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model.

    Physicochemical Properties

    M.Wt 485.41
    Formula C20H15F4N3O5S
    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-(((3S,4R)-1-((2-cyano-4-(trifluoromethyl)phenyl)sulfonyl)-4-hydroxy-4-(hydroxymethyl)pyrrolidin-3-yl)oxy)-2-fluorobenzonitrile

    References

    1. Brnardic EJ, et al. J Med Chem. 2018 Oct 18. doi: 10.1021/acs.jmedchem.8b01317.

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