CJ-15208

• CAT Number: I006148
• CAS Number: 210236-47-8
• Molecular Formula: C34H35N5O4
• Molecular Weight: 577.685
• Purity: ≥95%
• Synonyms: CJ-15208; CJ15208; CJ 15208; CJ-15,208; CJ15,208; CJ 15,208.c[Phe-D-Pro-Phe-Trp].;(3S,6S,9S,14aR)-6-((1H-indol-3-yl)methyl)-3,9-dibenzyldecahydropyrrolo[1,2-a][1,4,7,10]tetraazacyclododecine-1,4,7,10-tetraone
• Target: κ-opioid receptor antagonist
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term ,or -20 °C for long term
• SMILES: O=C(N1[C@H](CCC1)C(N[C@@H](CC2=CC=CC=C2)C(N[C@H]3CC4=CNC5=CC=CC=C54)=O)=O)[C@@H](NC3=O)CC6=CC=CC=C6

CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502. CJ-15208 was a selective binding inhibitor for the kappa opioid receptor: 47 nM (IC50) for kappa, 260 nM for mu, and 2,600 nM for delta. In the electrically-stimulated twitch response assay of rabbit vas deferens I recovered the suppression by a kappa agonist asimadoline with an ED50 of 1.3 microM, indicating that it is a kappa antagonist.

Reference

1:De Marco R, Bedini A, Spampinato S, Cavina L, Pirazzoli E, Gentilucci L. Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). J Med Chem. 2016 Sep 22. [Epub ahead of print] PubMed PMID: 27607020.