Formulation: A solid
Formal Name: N-(19-carboxy-1-oxononadecyl)-L-γ-glutamyl-L-lysyl-L-cysteinyl-L-asparaginyl-L-threonyl-L-alanyl-L-threonyl-L-cysteinyl-L-alanyl-L-threonyl-L-glutaminyl-L-arginyl-L-leucyl-L-alanyl-L-α-glutamyl-L-phenylalanyl-L-leucyl-L-arginyl-L-histidyl-L-seryl-L-seryl-L-asparaginyl-L-asparaginyl-L-phenylalanylglycyl-L-prolyl-L-isoleucyl-L-leucyl-L-prolyl-L-prolyl-L-threonyl-L-asparaginyl-L-valylglycyl-L-seryl-L-asparaginyl-L-threonyl-L-prolinamide, cyclic (3→8)-disulfide, acetate salt
Purity: ≥98%
Formula Markup: C194H312N54O59S2 • XC2H4O2
Formula Weight: 4409,1
Shelf life (days): 1460
Notes: 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}
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