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CJ-15208

Catalog No. T27027   CAS 210236-47-8
Synonyms: CJ15,208, CJ-15,208, CJ 15,208.c[Phe-D-Pro-Phe-Trp]

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

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CJ-15208 Chemical Structure
CJ-15208, CAS 210236-47-8
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CJ-15208 is a potent and selective κ-opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502 (IC50 are 47 nM for kappa, 260 nM for mu, and 2,600 nM for delta respectly). In the electrically-stimulated twitch response assay of rabbit vas deferens, CJ-15208 recovered the suppression by a kappa agonist asimadoline with an ED50 of 1.3 microM.
Synonyms CJ15,208, CJ-15,208, CJ 15,208.c[Phe-D-Pro-Phe-Trp]
Molecular Weight 577.67
Formula C34H35N5O4
CAS No. 210236-47-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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. 2. Khaliq T, Williams TD, Senadheera SN, Aldrich JV. Development of a robust, sensitive and selective liquid chromatography-tandem mass spectrometry assay for the quantification of the novel macrocyclic peptide kappa opioid receptor antagonist [D-Trp]CJ-15,208 in plasma and application to an initial pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Aug 15;1028:11-5. doi: 10.1016/j.jchromb.2016.05.043. Epub 2016 Jun 2. PubMed PMID: 27318293; PubMed Central PMCID: PMC4956519. 3. Aldrich JV, Senadheera SN, Ross NC, Reilley KA, Ganno ML, Eans SE, Murray TF, McLaughlin JP. Alanine analogues of [D-Trp]CJ-15,208: novel opioid activity profiles and prevention of drug- and stress-induced reinstatement of cocaine-seeking behaviour. Br J Pharmacol. 2014 Jul;171(13):3212-22. doi: 10.1111/bph.12664. PubMed PMID: 24588614; PubMed Central PMCID: PMC4080975. 4. Bidlack JM. Mixed κ/μ partial opioid agonists as potential treatments for cocaine dependence. Adv Pharmacol. 2014;69:387-418. doi: 10.1016/B978-0-12-420118-7.00010-X. Review. PubMed PMID: 24484983.

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Keywords

CJ-15208 210236-47-8 CJ15,208 CJ-15,208 CJ 15,208.c[Phe-D-Pro-Phe-Trp] CJ15208 CJ 15208 inhibitor inhibit

 

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