MK-8318

MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Inflammation/Immunology

CRTH2/DP2 Receptor:5.0 nM (Ki)

β-arrestin:3.5 nM (IC50)

cAMP:8.0 nM (IC50)

CYP3A4:50 μM (IC50)

CYP2C9:50 μM (IC50)

CYP2D6:50 μM (IC50)

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 mpk. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy[1].

[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.

Dinoprostone | Prostaglandin E1 | E7046 | ONO-AE3-208 | PF 04418948 | Fevipiprant | grapiprant | TG6-10-1 | Taprenepag | GW 627368 | MRE-269 | Ramatroban | AH 6809 | Laropiprant | AZD1981