MK-8318 |
| Catalog No.GC31851 |
MK-8318은 Ki가 5.0nM인 강력하고 선택적인 CRTh2 수용체 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1416581-40-2
Sample solution is provided at 25 µL, 10mM.
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MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
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[1].
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].
[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.
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