MK-8318 

MK-8318 is a potent and selective CRTh2 receptor antagonist with a K_i of 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

534.50

C₂₇H₂₆F₄N₂O₅

1416581-40-2

FC1=CC=C(N(C(C2=CC=C(OC(F)(F)F)C=C2)=O)[C@@H](CCC3)[C@@H]3[C@H]4N(C(CCC(O)=O)=O)C5CC5)C4=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Huang X, et al. Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684.  [Content Brief]