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AZD 5462 is an agonist of relaxin family peptide receptor 1 (RXFP1).1 It induces cAMP mobilization in HEK293 cells expressing the human RXFP1 (EC50 = 15.85 nM). AZD 5462 increases heart rate and mean arterial blood pressure (MABP) in rats. It increases left ventricular ejection fraction (LVEF) in a cynomolgus monkey model of heart failure induced by a high-fat diet and age when administered at doses of 1 or 10 mg/kg per day.
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1. Discovery of clinical candidate AZD5462, a selective oral allosteric RXFP1 agonist for treatment of heart failure. J. Med. Chem. 67(6), 4419-4441 (2024).