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MK-8825

Chemical Structure : MK-8825

CAS No.: 1380887-60-4

MK-8825 (MK8825)

Catalog No.: PC-62994Not For Human Use, Lab Use Only.

MK-8825 is a highly potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 17 nM for rat CGRP.

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    Biological Activity

    MK-8825 is a highly potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 17 nM for rat CGRP.
    MK-8825 blocks hCGRP-stimulated cAMP responses in HEK293 cells stably expressing the human CGRP receptor with IC50 of 0.23 nM.
    MK-8825 possesses significantly improved in vivo potency in rat pharmacodynamic models.

    Physicochemical Properties

    M.Wt 572.617
    Formula C31H30F2N6O3
    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

    2-[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(6S)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridin]-3-yl]acetamide

    References

    1. Bell IM, et al. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3941-5.

    2. Michot B, et al. Eur J Pain. 2015 Feb;19(2):281-90.

    3. Romero-Reyes M, et al. Exp Neurol. 2015 Sep;271:95-103.

    4. Feistel S, et al. J Headache Pain. 2013 Nov 20;14:93.

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