MK-8318

Modify Date: 2024-01-31 18:38:41

MK-8318 Structure
MK-8318 structure
Common Name MK-8318
CAS Number 1416581-40-2 Molecular Weight 534.50
Density N/A Boiling Point N/A
Molecular Formula C27H26F4N2O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MK-8318


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

 Names

Name MK-8318

 MK-8318 Biological Activity

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

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)

In Vitro 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 Vivo 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C27H26F4N2O5
Molecular Weight 534.50