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Description: GSK-269984A is a novel and potent Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9. GSK269984A was designed to overcome development issues encountered with previous EP(1) antagonists such as GW848687X and was found to display excellent activity in preclinical models of inflammatory pain. However, upon cross species pharmacokinetic profiling, GSK269984A was predicted to have suboptimal human pharmacokinetic and was thus progressed to a human microdose study.
References: Bioorg Med Chem Lett. 2009 May 1; 19(9):2599-603.
Related CAS#:892664-17-4 (GSK-269984B)
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