CYN 154806 (TFA)

CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively[1][2].

Product Specifications

CAS Number

[2828432-46-6]

UNSPSC

12352209

Target

Somatostatin Receptor

Type

Peptides

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/cyn-154806-tfa.html

Purity

99.81

Solubility

H2O : 25 mg/mL (ultrasonic)

Smiles

O=C([C@@H](NC([C@@H](CSSC[C@H](NC([C@](NC([C@@H](NC1=O)CCCCN)=O)([H])[C@H](O)C)=O)C(N[C@@H](C(N)=O)CC2=CC=C(C=C2)O)=O)NC([C@@H](NC(C)=O)CC3=CC=C(C=C3)[N+]([O-])=O)=O)=O)CC4=CC=C(C=C4)O)N[C@@H]1CC5=CNC6=CC=CC=C56.OC(C(F)(F)F)=O

Molecular Formula

C58H69F3N12O16S2

Molecular Weight

1311.36

References & Citations

[1]Bass RT, et al. Identification and characterization of novel somatostatin antagonists. Mol Pharmacol. 1996 Oct;50 (4) :709-15.|[2]Feniuk W, et al. Selective somatostatin sst (2) receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology. 2000 Jun 8;39 (8) :1443-50.|[3]Takeuchi K, et al. Activation of Muscarinic Acetylcholine Receptor Subtype 4 Is Essential for Cholinergic Stimulation of Gastric Acid Secretion: Relation to D Cell/Somatostatin. Front Pharmacol. 2016 Aug 30;7:278.