For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.<br>IC50 value:<br>Target: CB1 receptor<br>Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24). Org 27569 significantly increases binding of the CB1 agonist [3H]CP 55.940 (pKb = 5.67) and decreases binding of the CB1 inverse agonist [3H]SR 141716A (pKb = 5.95). Org 27569 inhibits CB1 receptor antagonist efficacy in vitro (pKb = 7.57).</p>
| Catalog Number | I005224 |
| CAS Number | 868273-06-7 |
| Synonyms | 5-chloro-3-ethyl-N-[2-(4-piperidin-1-ylphenyl)ethyl]-1H-indole-2-carboxamide |
| Molecular Formula | C24H28ClN3O |
| Purity | ≥95% |
| Target | Cannabinoid Receptor |
| Solubility | DMSO: ≥ 52.2 mg/mL |
| Storage | 3 years -20C powder |
| Reference | </br>1:Effects of the cannabinoid CB₁ receptor allosteric modulator ORG 27569 on reinstatement of cocaine- and methamphetamine-seeking behavior in rats. Jing L, Qiu Y, Zhang Y, Li JX.Drug Alcohol Depend. 2014 Oct 1;143:251-6. doi: 10.1016/j.drugalcdep.2014.08.004. Epub 2014 Aug 17. PMID: 25169627 Free PMC Article</br>2:In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569. Gamage TF, Ignatowska-Jankowska BM, Wiley JL, Abdelrahman M, Trembleau L, Greig IR, Thakur GA, Tichkule R, Poklis J, Ross RA, Pertwee RG, Lichtman AH.Behav Pharmacol. 2014 Apr;25(2):182-5. doi: 10.1097/FBP.0000000000000027. PMID: 24603340 Free PMC Article</br>3:A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569. Fay JF, Farrens DL.J Biol Chem. 2012 Sep 28;287(40):33873-82. Epub 2012 Jul 30. PMID: 22846992 Free PMC Article |
