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MK-8318

Chemical Structure : MK-8318

CAS No.: 1416581-40-2

MK-8318 (MK8318)

Catalog No.: PC-35509Not For Human Use, Lab Use Only.

MK-8318 (MK8318) is a potent, selective, orally available CRTh2 receptor antagonist with Ki of 5 nM, shows nM potency in functional assay (cAMP IC50=8 nM, β-Arrestin IC50=3.5 nM.

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    Biological Activity

    MK-8318 (MK8318) is a potent, selective, orally available CRTh2 receptor antagonist with Ki of 5 nM, shows nM potency in functional assay (cAMP IC50=8 nM, β-Arrestin IC50=3.5 nM.
    MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mpk, also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mpk oral dosing.
    MK-8318 exhibits a favorable PK profile suitable for once daily oral dosing for potential treatment of asthma.

    Physicochemical Properties

    M.Wt 534.508
    Formula C27H26F4N2O5
    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-(cyclopropyl((3aS,9R,9aR)-7-fluoro-4-(4-(trifluoromethoxy)benzoyl)-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl)amino)-4-oxobutanoic acid

    References

    1. Huang X, et al. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684.

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