Cortistatin-14 (trifluoroacetate salt)

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). It is expressed in GABAergic interneurons in the cortex and hippocampus. Cortistatin-14 competitively inhibits hexarelin binding to human growth hormone secretagogue receptors (GHS-R) in pituitary membranes (Ki = 0.54 µM). It also activates the human Mas-related gene receptor MrgX2 expressed in HEK293 cells leading to quantifiable GTP-gammaS binding to the G protein subunit Galphaomega (EC50 = 1.3 µM). Cortistatin-14 (0.01-1 µM), similarly to somatostatin-14 (Cay-20809), completely inhibits thyrotropin-releasing hormone (TRH, Cay-22917), and partially inhibits vasoactive intestinal peptide (VIP, Cay-24996), stimulation of cAMP production in GH4 cells. In mice, cortistatin-14 dose-dependently (0.05-5 µg, i.c.v.) impairs memory retention when administered after foot shock avoidance training. 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.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. Molecular Formula: C81H113N19O19S2 . XCF3COOH. Formula Weight: 1721.0. Purity: >95%. Formulation: (Request formulation change), A lyophilized powder. Solubility: Water: 1 mg/ml. SMILES: [H]N1CCC[C@H]1C(N[C@H](C(N[C@@H](CCCCN)C(N[C@@H](CC(N)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CCCCN)C(N[C@]([C@@H](C)O)([H])C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CO)C2=O)=O)=O)CC3=CC=CC=C3)=O)=O)=O)CC4=CNC5=C4C=CC=C5)=O)CC6=CC=CC=C6)=O)CC7=CC=CC=C7)=O)=O)=O)CSSC[C@H](N2)C(N[C@@H](CCCCN)C(O)=O)=O)=O.FC(F)(C(O)=O)F. InChi Code: InChI=1S/C81H113N19O19S2.C2HF3O2/c1-46(103)67-80(117)95-59(38-49-24-9-4-10-25-49)73(110)96-62(42-101)76(113)97-63(43-102)77(114)99-65(79(116)90-56(81(118)119)30-15-18-34-84)45-121-120-44-64(98-68(105)53-31-19-35-86-53)78(115)89-54(28-13-16-32-82)69(106)94-61(40-66(85)104)75(112)92-57(36-47-20-5-2-6-21-47)71(108)91-58(37-48-22-7-3-8-23-48)72(109)93-60(39-50-41-87-52-27-12-11-26-51(50)52)74(111)88-55(70(107)100-67)29-14-17-33-83,3-2(4,5)1(6)7/h2-12,20-27,41,46,53-65,67,86-87,101-103H,13-19,28-40,42-45,82-84H2,1H3,(H2,85,104)(H,88,111)(H,89,115)(H,90,116)(H,91,108)(H,92,112)(H,93,109)(H,94,106)(H,95,117)(H,96,110)(H,97,113)(H,98,105)(H,99,114)(H,100,107)(H,118,119),(H,6,7)/t46-,53+,54+,55+,56+,57+,58+,59+,60+,61+,62+,63+,64+,65+,67+,/m1./s1. InChi Key: CXQSAJNOSPDIQD-BJUJOSGCSA-N.