Org 27569
Org 27569 is an allosteric ligand of the cannabinoid receptor CB1[1].
Org 27569 has been reported to promote the agonist CP55940 binding to purified bimane-labeled CB1 receptor and act directly on the CB1 receptor, yet at the same time inhibit receptor function. In addition, org 27569 has shown the potent inhibition of electrically evoked contractions of the mouse vas deferens by WIN55212 with the pEC50 and Emax of 8.24 ±0.12 and 45.4%, respectively. Apart from these, the pKB and Logα values for org 27569 at the putative allosteric site on the CB1 receptor are 5.67±0.23 and 1.14±0.17, respectively[1, 2].
References:
[1] Price MR1, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G, Westwood P, Marrs J, Thomson F, Cowley P, Christopoulos A, Pertwee RG, Ross RA. Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol. 2005 Nov;68(5):1484-95. Epub 2005 Aug 19.
[2] Fay JF1, Farrens DL. A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569. J Biol Chem. 2012 Sep 28;287(40):33873-82. Epub 2012 Jul 30.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 409.95 |
| Cas No. | 868273-06-7 |
| Formula | C24H28ClN3O |
| Solubility | insoluble in H2O; ≥13.95 mg/mL in DMSO; ≥2.22 mg/mL in EtOH |
| Chemical Name | 5-chloro-3-ethyl-N-[2-(4-piperidin-1-ylphenyl)ethyl]-1H-indole-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | Org 27569 is an allosteric modulator of cannabinoid CB1 receptor | |||||
| Targets | CB1 | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
