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Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.
OBESITY RESEARCH SOLUTIONSCagrilintide is an agonist of amylin and calcitonin receptors and an acylated derivative of amylin.1,2 It binds to the amylin 3 receptor (AMY3; IC50 = 170 pM for the human receptor) and calcitonin receptor (IC50 = 223 pM for the human receptor). Cagrilintide activates human AMY3 and calcitonin receptors in reporter assays (EC50s = 49 and 62 pM, respectively). It increases cAMP accumulation in COS-1 cells expressing AMY1, AMY3, or calcitonin receptors (EC50s = 79.43, 114.82, and 43.65 nM, respectively).2 Cagrilintide (250 µM) has a low propensity for inducing amyloid fibril formation with a lag time of 45 hours in a thioflavin T assay.1 Cagrilintide reduces food intake in rats for at least 48 hours after administration of a single dose of 3 or 30 nmol/kg. It reduces body weight, food intake, and fat mass, but does not reduce blood glucose or increase blood insulin levels, in a mouse model of diet-induced obesity when administered at a dose of 100 nmol/kg.3
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1. Development of cagrilintide, a long-
2. AM833 is a novel agonist of calcitonin family G protein-
3. Identification and utility exploration of a highly potent and long-