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AS1928370

Chemical Structure : AS1928370

CAS No.: 1345614-89-2

AS1928370 (ASP-8370;ASP8370)

Catalog No.: PC-35235Not For Human Use, Lab Use Only.

AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM.

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

    Biological Activity

    AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM.
    AS1928370 (ASP8370) demonstrates high aqueous solubility (pH6.8, >100 uM), satisfactory stability in human liver microsomes, and reduced CYP3A4 inhibition.
    AS1928370 (ASP8370) improves capsaicin-induced secondary hyperalgesia and mechanical allodynia in an L5/L6 spinal nerve ligation model in rats with respective ED50s of 0.17 and 0.26 mg/kg p.o.

    Physicochemical Properties

    M.Wt 453.586
    Formula C29H31N3O2
    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

    (R)-N-(1-methyl-2-oxo-1,2,3,4-tetrahydro-7-quinolyl)-2-[(2-methylpyrrolidin-1-yl)methyl]biphenyl-4-carboxamide

    References

    1. Oka H, et al. Bioorg Med Chem. 2018 Jul 23;26(12):3716-3726.

    2. Watabiki T, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):743-50.

    3. Watabiki T, et al. Biol Pharm Bull. 2011;34(7):1105-8.

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