MK-8318 is a potent and selectiveCRTh2 receptorantagonist with a K_iof 5.0 nM.

MK-8318 also inhibits β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 with IC₅₀s of 3.5±2.1 nM, 8.0±6.8 nM, 50 μM, 50 μM and 50 μM^[1].

In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mg/kg. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy. MK-8318 also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing^[1].

534.50

C₂₇H₂₆F₄N₂O₅

1416581-40-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.