Home GPCR & G Protein Cannabinoid Receptor agonist Org 27569

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Org 27569 Cannabinoid Receptor agonist

Cat.No.S1534

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.
Org 27569 Cannabinoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 409.95

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Quality Control

Batch: S153401 DMSO]82 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.72%
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99.72

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 409.95 Formula

C24H28ClN3O

 Storage (From the date of receipt)
CAS No. 868273-06-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4

Mechanism of Action

Features
Traps the receptor in a distinct agonist-bound, but non-signaling conformational state.
Targets/IC50/Ki
CB1
In vitro
Org 27569 is an allosteric modulator of CB1 cannabinoid receptor. It significantly increases the binding of CB1 receptor agonist and causes a significant decrease in specific binding of CB1 receptor inverse agonist. This compound induces CB1 high affinity agonist binding, receptor internalization, and downstream ERK phosphorylation. The allosteric ligand promotes agonist binding to CB1, yet blocks the agonist-induced conformational changes in TM6. It traps the receptor in a distinct agonist-bound, but nonsignaling conformational state.
Kinase Assay
Equilibrium Binding Assays.
Binding assays are performed with the CB1 receptor agonist [3H]CP 55,940 (0.7 nM) and the CB1 receptor antagonist [3H]SR 141716A (1.2 nM), 1 mg/ml BSA and 50 mM Tris buffer containing 0.1 mM EDTA and 0.5 mM MgCl2, pH 7.4, in a total assay volume of 500 μl. Binding is initiated by the addition of mouse brain membranes (30 μg). Assays are carried out at 37°C for 60 min before termination by addition of ice-cold wash buffer (50 mM Tris buffer and 1 mg/ml BSA) and vacuum filtration using a 24-well sampling manifold and Whatman GF/B glass-fiber filters that have been soaked in wash buffer at 4°C for 24 h. Each reaction tube is washed five times with a 4-ml aliquot of buffer. The filters are oven-dried for 60 min and then placed in 5 ml of scintillation fluid, and radioactivity is quantitated by liquid scintillation spectrometry. Specific binding is defined as the difference between the binding that occurred in the presence and absence of 1 μM concentrations of the corresponding unlabeled ligand and is 70 to 80% of the total binding.
References

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