MK-8318 | CRTH2 inhibitor | Probechem Biochemicals

Chemical Structure : MK-8318

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MK-8318 (MK8318)

货号: PC-35509Not For Human Use, Lab Use Only.

MK-8318 (MK8318) is a potent, selective, orally available CRTh2 receptor antagonist with Ki of 5 nM, shows nM potency in functional assay (cAMP IC50=8 nM, β-Arrestin IC50=3.5 nM.

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生物&药学活性

MK-8318 (MK8318) is a potent, selective, orally available CRTh2 receptor antagonist with Ki of 5 nM, shows nM potency in functional assay (cAMP IC50=8 nM, β-Arrestin IC50=3.5 nM.
MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mpk, also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mpk oral dosing.
MK-8318 exhibits a favorable PK profile suitable for once daily oral dosing for potential treatment of asthma.

物理化学性质&存储条件

分子量	534.508
分子式	C27H26F4N2O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(cyclopropyl((3aS,9R,9aR)-7-fluoro-4-(4-(trifluoromethoxy)benzoyl)-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl)amino)-4-oxobutanoic acid

参考文献

1. Huang X, et al. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684.

MK-8318 (MK8318)

生物&药学活性

物理化学性质&存储条件

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MK-8318 (MK8318)

生物&药学活性

物理化学性质&存储条件

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