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Chemical Structure : MK-8318
Catalog No.: 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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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; 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.
| M.Wt | 534.508 | |
| Formula | C27H26F4N2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Huang X, et al. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684.
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