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GR127935

Chemical Structure : GR127935

CAS No.: 148672-13-3

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GR127935 (GR-127935)

Catalog No.: PC-61865Not For Human Use, Lab Use Only.

GR127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.

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

    Biological Activity

    GR127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.
    GR127935 displays >100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types.
    GR127935 blocks porcine carotid vascular response to sumatriptan in vivo; orally bioavailable and centrally active.

    Physicochemical Properties

    M.Wt 497.587
    Formula C29H31N5O3
    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

    N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide

    References

    1. Clitherow JW, et al. J Med Chem. 1994 Jul 22;37(15):2253-7.

    2. Knobelman DA, et al. J Pharmacol Exp Ther. 2001 Sep;298(3):1083-91.

    3. De Vries P, et al. Br J Pharmacol. 1996 May;118(1):85-92.

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