产品描述:
Cagrilintide is an agonist of amylin and calcitonin receptors and an acylated derivative of amylin.{51846,51847} 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).{51847} Cagrilintide (250 µM) has a low propensity for inducing amyloid fibril formation with a lag time of 45 hours in a thioflavin T assay.{51846} 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.{51848}