Name | MK-8318 |
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Description | MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM. |
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Related Catalog | |
Target |
CRTH2/DP2 Receptor: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) |
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[1]. |
In Vivo | In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mpk. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy[1]. |
References |
Molecular Formula | C27H26F4N2O5 |
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Molecular Weight | 534.50 |