| Identification | Back Directory | [Name]
MK-8318 | [CAS]
1416581-40-2 | [Synonyms]
MK-8318
Butanoic acid, 4-[cyclopropyl[(3aS,9R,9aR)-7-fluoro-2,3,3a,4,9,9a-hexahydro-4-[4-(trifluoromethoxy)benzoyl]-1H-cyclopenta[b]quinolin-9-yl]amino]-4-oxo- | [Molecular Formula]
C27H26F4N2O5 | [MDL Number]
MFCD31807606 | [MOL File]
1416581-40-2.mol | [Molecular Weight]
534.5 |
| Hazard Information | Back Directory | [Description]
MK-8318 is potent and selective CRTh2 antagonist activity and a favorable PK profile suitable for once daily oral dosing for potential treatment of asthma. MK-8318 showed good in vitro and in vivo activity (Ki = 2.3 nM; IC50 cAMP = 8 nM). | [Uses]
MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM. | [in vivo]
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]. | [IC 50]
DP: 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) | [storage]
Store at -20°C | [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. DOI:10.1021/acsmedchemlett.8b00145 |
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