Formulation: A lyophilized powder
Formal Name: L-prolyl-L-cysteinyl-L-lysyl-L-asparaginyl-L-phenylalanyl-L-phenylalanyl-L-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-L-seryl-L-seryl-L-cysteinyl-L-lysine, cyclic (2→13)-disulfide, trifluoroacetate salt
Purity: ≥95%
Formula Markup: C81H113N19O19S2 • XCF3COOH
Formula Weight: 1721
Shelf life (days): 1460
Notes: Cortistatin-14 is an endogenous neuropeptide agonist of somatostatin receptors (IC50s = 0.5-18.2 nM for human SST1-SST5 receptors expressed in CCL39 cells).{41724,38847} It is expressed in GABAergic interneurons in the cortex and hippocampus.{38847,38846} Cortistatin-14 competitively inhibits hexarelin binding to human growth hormone secretagogue receptors (GHS-R) in pituitary membranes (Ki = 0.54 μM).{41725} It also activates the human Mas-related gene receptor MrgX2 expressed in HEK293 cells leading to quantifiable GTP-γS binding to the G protein subunit Gαο (EC50 = 1.3 μM).{41726} Cortistatin-14 (0.01-1 μM), similarly to somatostatin-14 (Item No. 20809), completely inhibits thyrotropin-releasing hormone (TRH; Item No. 22917), and partially inhibits vasoactive intestinal peptide (VIP; Item No. 24996), stimulation of cAMP production in GH4 cells.{38846} In mice, cortistatin-14 dose-dependently (0.05-5 μg, i.c.v.) impairs memory retention when administered after foot shock avoidance training.{41727} Cortistatin-14 (40-320 μg/kg, s.c.) dose-dependently reduces growth hormone secretion in rats by greater than 80% after 10 minutes when administered at doses of 40-320 µg/kg.{41728}
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