A neuropeptide agonist of somatostatin receptors
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Cortistatin-14 (trifluoroacetate salt)

Item No. 25074

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    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).1,2 It is expressed in GABAergic interneurons in the cortex and hippocampus.2,3 Cortistatin-14 competitively inhibits hexarelin binding to human growth hormone secretagogue receptors (GHS-R) in pituitary membranes (Ki = 0.54 μM).4 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).5 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.3 In mice, cortistatin-14 dose-dependently (0.05-5 μg, i.c.v.) impairs memory retention when administered after foot shock avoidance training.6 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.7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Criado, J.R., Li, H., Jiang, X., et al. Structural and compositional determinants of cortistatin activity. J. Neurosci. Res. 56(6), 611-619 (1999).

    2. Spier, A.D., and de Lecea, L. Cortistatin: A member of the somatostatin neuropeptide family with distinct physiological functions. Brain Res. Brain Res. Rev. 33(2-3), 228-241 (2000).

    3. de Lecea, L., Criado, J.R., Prospero-Garcia, O., et al. A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature 381(6579), 242-245 (1996).

    4. Deghenghi, R., Papotti, M., Ghigo, E., et al. Cortistatin, but not somatostatin, binds to growth hormone secretagogue (GHS) receptors of human pituitary gland. J. Endocrinol. Invest. 24(1), RC1-RC3 (2001).

    5. Burstein, E.S., Ott, T.R., Feddock, M., et al. Characterization of the Mas-related gene family: structural and functional conservation of human and rhesus MrgX receptors. Br. J. Pharmacol. 147(1), 73-82 (2006).

    6. Flood, J.F., Uezu, K., and Morley, J.E. The cortical neuropeptide, cortistatin-14, impairs post-training memory processing. Brain Res. 775(1-2), 250-252 (1997).

    7. Deghenghi, R., Avallone, R., Torsello, A., et al. Growth hormone-inhibiting activity of cortistatin in the rat. J. Endocrinol. Invest. 24(11), RC31-RC33 (2001).