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Casopitant mesylate

Chemical Structure : Casopitant mesylate

CAS No.: 414910-30-8

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Casopitant mesylate (GW679769B, GW679769 mesylate)

Catalog No.: PC-61581Not For Human Use, Lab Use Only.

Casopitant (GW679769) mesylate is a potent, selective, orally active, and brain penetrant neurokinin 1 (NK1) receptor antagonist with pKi of 9.48.

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

    Biological Activity

    Casopitant (GW679769) mesylate is a potent, selective, orally active, and brain penetrant neurokinin 1 (NK1) receptor antagonist with pKi of 9.48.
    Casopitant (GW679769) inhibit SP-induced release of cytosolic Ca2+ in h-NK1-CHO cells using FLIPR with pA2 value of 9.7.
    Casopitant (GW679769) possesses subnanomolar affinity and high selectivity for the NK1 receptors without sign of pharmacological species difference between human and gerbil NK1 receptors.
    Casopitant (GW679769) possesses an anxiolytic-like property, confirming the preclinical profile of NK1 receptor antagonists on emotional behavior.

    Physicochemical Properties

    M.Wt 712.725
    Formula C31H39F7N4O5S
    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

    (2R,4S)-4-(4-acetylpiperazin-1-yl)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methylpiperidine-1-carboxamide mesylate

    References

    1. Minthorn E, et al. Drug Metab Dispos. 2008 Sep;36(9):1846-52.

    2. Ruhlmann C, et al. Ther Clin Risk Manag. 2009 Apr;5(2):375-84.

    3. Singla NK, et al. Anesthesiology. 2010 Jul;113(1):74-82.

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