Org 27569

Org 27569

Catalog Number:
FC01365274APE
Mfr. No.:
APE-B1426
Price:
$247
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          Background

          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].

          [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.

      • Properties
        • Categories
          Cannabinoid CB1 receptor allosteric modulator
          Alternative Name
          5-chloro-3-ethyl-N-[2-(4-piperidin-1-ylphenyl)ethyl]-1H-indole-2-carboxamide
          CAS Number
          868273-06-7
          Molecular Formula
          C24H28ClN3O
          Molecular Weight
          409.95
          Appearance
          A solid
          Purity
          99.33%
          Solubility
          insoluble in H2O; ≥13.95 mg/mL in DMSO; ≥2.22 mg/mL in EtOH
          Storage
          Store at -20°C
          SMILES
          CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4

          * For Research Use Only

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