MK-8318,1416581-40-2

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MK-8318

CAS No. : 1416581-40-2

MCE 国际站：MK-8318

产品活性：MK-8318 是一种有效的选择性 CRTh2 受体拮抗剂，K_i 为 5.0 nM。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

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.

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.

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