TargetMol

CJ-15208

Product Code:
 
TAR-T27027
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T27027-5mg5mg£850.00
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Further Information

Bioactivity:
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.
CAS:
210236-47-8
Formula:
C34H35N5O4
Molecular Weight:
577.685
Purity:
0.98
SMILES:
O=C1N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@H]12

References

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 ?/? 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.