Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593465 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
The recently discovered apelin/APJ system has emerged as a critical mediator of cardiovascular homeostasis and is associated with the pathogenesis of cardiovascular disease. A role for apelin/APJ in energy metabolism and gastrointestinal function has also recently emerged. We disclose the discovery and characterization of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221), a potent APJ functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor.
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Authors
Patrick R. Maloney, Pasha Khan, Michael Hedrick, Palak Gosalia, Monika Milewski, Linda Li, Gregory P. Roth, Eduard Sergienko, Eigo Suyama, Eliot Sugarman, Kevin Nguyen, Alka Mehta, Stefan Vasile, Ying Su, Derek Stonich, Hung Nguyen, Fu-Yue Zeng,