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MK-7246

 
National Institutes of Health

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2019
2019
Synthesis and preclinical evaluation of the CRTH2 antagonist [11C]MK-7246 as a novel PET tracer and potential surrogate marker for pancreatic beta-cell mass.
INTRODUCTION MK-7246 is a potent and selective antagonist for chemoattractant receptor-homologous molecule expressed on Th2 cells… Expand
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2014
2014
Anti-inflammatory actions of Chemoattractant Receptor-homologous molecule expressed on Th2 by the antagonist MK-7246 in a novel rat model of Alternaria alternata elicited pulmonary inflammation.
Alternaria alternata is a fungal allergen linked to the development of severe asthma in humans. In view of the clinical… Expand
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2013
2013
Pharmacological characterization of the late phase reduction in lung functions and correlations with microvascular leakage and lung edema in allergen-challenged Brown Norway rats.
Late phase airflow obstruction and reduction in forced vital capacity are characteristic features of human asthma. Airway… Expand
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2012
2012
UGT2B17 Genetic Polymorphisms Dramatically Affect the Pharmacokinetics of MK-7246 in Healthy Subjects in a First-in-Human Study
MK-7246, an antagonist of the chemoattractant receptor on T helper type 2 (Th2) cells, is being developed for the treatment of… Expand
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2012
2012
CRTH2 antagonist MK-7246: a synthetic evolution from discovery through development.
In this paper, we report the development of different synthetic routes to MK-7246 (1) designed by the Process Chemistry group… Expand
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2011
2011
Pharmacological Characterization of MK-7246, a Potent and Selective CRTH2 (Chemoattractant Receptor-Homologous Molecule Expressed on T-Helper Type 2 Cells) Antagonist
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor that… Expand
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2011
2011
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies… Expand
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2011
2011
Azaindoles as potent CRTH2 receptor antagonists.
A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the… Expand
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