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Description: MK-7246 is a novel, potent and selective CRTH2 antagonist with Ki of 2.5+/-0.5 nM. MK-7246 has high affinity for the human, monkey, dog, rat, and mouse CRTH2, it interacts with CRTH2 in a reversible manner, it exhibits high selectivity over all prostanoid receptors as well as 157 other receptors and enzymes, it acts as a full antagonist on recombinant and endogenously expressed CRTH2, it demonstrates good oral bioavailability and metabolic stability in various animal species, it yields ex vivo blockade of CRTH2 on eosinophils in monkeys and sheep, and it significantly blocks antigen-induced late-phase bronchoconstriction and airway hyper-responsiveness in sheep. MK-7246 represents a potent and selective tool to further investigate the in vivo function of CRTH2.
References: Mol Pharmacol. 2011 Jan; 79(1):69-76.
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