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Submit ReviewCYN 154806 is a potent and selective somatostatin sst2 receptor antagonist. pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
M. Wt | 1197.35 |
Formula | C56H68N12O14S2 |
Sequence |
FCYWKTCY (Modifications: Phe-1 = Ac-(4-nitro)Phe, Cys-2 = D-Cys, Trp-4 = D-Trp, Tyr-8 = D-Tyr & C-terminal amide, Disulfide bridge: 2-7) |
Storage | Store at -20°C |
Purity | ≥95% (HPLC) |
CAS Number | 183658-72-2 |
PubChem ID | 16133842 |
InChI Key | RDTVTSXTFYXNSG-HDNDNHAUSA-N |
Smiles | C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@@H](CSSC[C@H](NC1=O)C(=O)N[C@H](CC1=CC=C(O)C=C1)C(N)=O)NC(=O)[C@H](CC1=CC=C(C=C1)[N+]([O-])=O)NC(C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility | Soluble to 1 mg/ml in water |
References are publications that support the biological activity of the product.
Bass et al (1996) Identification and characterization of novel somatostatin antagonists. Mol.Pharmacol. 50 709 PMID: 8863814
Feniuk et al (2000) Selective somatostatin sst2 receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology 39 1443 PMID: 10818260
Hannon et al (2002) Drug design at peptide receptors. Somatostatin receptor ligands. J.Mol.Neurosci. 18 15 PMID: 11931345
If you know of a relevant reference for CYN 154806, please let us know.
Keywords: CYN 154806, CYN 154806 supplier, Selective, sst2, antagonists, Receptors, Somatostatin, CYN154806, 1843, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for CYN 154806 include:
Foong et al (2010) 5-HT(1A), SST(1), and SST(2) receptors mediate inhibitory postsynaptic potentials in the submucous plexus of the guinea pig ileum. Neuroimmunomodulation 298 G384 PMID: 20007849
Paramonov et al (2018) Targeting Somatostatin Receptors By Functionalized Mesoporous Silica Nanoparticles - Are We Striking Home?. Nanotheranostics 2 320 PMID: 30148051
Hastoy et al (2018) Electrophysiological properties of human beta-cell lines EndoC-βH1 and -βH2 conform with human beta-cells. Sci Rep 8 16994 PMID: 30451893
Elliott et al (2015) Somatostatin and Ins mediate glucose-inhibited glucagon secretion in the pancreatic α-cell by lowering cAMP. Am J Physiol Endocrinol Metab 308 E130 PMID: 25406263
Spitsin et al (2013) Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor. J Leukoc Biol 20 247 PMID: 23921645
Bowman et al (2019) Somatostatin 2 Receptors in the Spinal Cord Tonically Restrain Thermogenic, Cardiac and Other Sympathetic Outflows. Front Neurosci 13 121 PMID: 30842723
Iwagaki et al (2013) Neurochemical characterisation of lamina II inhibitory interneurons that express GFP in the PrP-GFP mouse. Mol Pain 9 56 PMID: 24176114
Yang et al (2010) Activation of submucosal 5-HT(3) receptors elicits a somatostatin-dependent inhibition of ion secretion in rat colon. Br J Pharmacol 159 1623 PMID: 20233224
Do you know of a great paper that uses CYN 154806 from Tocris? Please let us know.
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