Org 27569 is a CB1 receptor allosteric modulator. Exhibits increased binding of the CB1 agonist. Inhibits CB1 receptor antagonist effectiveness in vitro.Potent CB 1 receptor allosteric modulator (pEC 50 = 8.24). Significantly increases binding of the CB 1
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR
Mechanism of action
Allosteric modulator of CB 1 receptor
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
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. A CB1 receptor allosteric modulator.
1.Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G et al.. (2005) Allosteric modulation of the cannabinoid CB1 receptor.. Mol Pharmacol, 68 (5):(1484-95). [PMID:16113085][10.1021/op500134e]
2.Fay JF, Farrens DL. (2012) A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569.. J Biol Chem, 287 (40):(33873-82). [PMID:22846992][10.1021/op500134e]
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