产品
编 号：F645390
分子式：C27H26F4N2O5
分子量：534.5
分子式：C27H26F4N2O5
分子量：534.5
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CAS No: 1416581-40-2
产品详情
生物活性：
MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
体内研究：
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.
体外研究：
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.
MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
体内研究：
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.
体外研究：
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.
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