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Org 27569

Catalog No.
B1426
Cannabinoid CB1 receptor allosteric modulator
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$92.00
In stock
10mg
$79.00
In stock
50mg
$329.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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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].

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt409.95
Cas No.868273-06-7
FormulaC24H28ClN3O
Solubility≥13.95mg/mL in DMSO
Chemical Name5-chloro-3-ethyl-N-[2-(4-piperidin-1-ylphenyl)ethyl]-1H-indole-2-carboxamide
SDFDownload SDF
Canonical SMILESCCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Org 27569 is an allosteric modulator of cannabinoid CB1 receptor
Targets CB1          
IC50            

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