1416581-40-2

Name	MK-8318
CAS	1416581-40-2
Molecular Formula	C27H26F4N2O5
MDL Number	MFCD31807606
Molecular Weight	534.5
MOL File	1416581-40-2.mol

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-

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Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO

Hazard Information

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

Supplier

RD International Technology Co., Limited

Telephone 18024082417

Websitehttps://www.ruidiresearch.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Biosynth Biological Technology (Suzhou) Co Ltd

Telephone 51288865780

Websitehttp://www.biosynth.com

Adooq Bioscience LLC

Telephone400-025-6535

Websitehttp://www.adooq.cn

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