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Org 27569

Name: Org 27569
Brand: Selleck Chemicals
SKU: S1534
Rating: 5 (1 reviews)

Catalog No.S1534

For research use only.

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.

CAS No. 868273-06-7

Selleck's Org 27569 has been cited by 1 Publication

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Cannabinoid Receptor Signaling Pathway Map

Biological Activity

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.

Features

Traps the receptor in a distinct agonist-bound, but non-signaling conformational state.

Targets

CB1 ^[2]

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. ^[1] Org 27569 induces CB1 high affinity agonist binding, receptor internalization, and downstream ERK phosphorylation. ^[2] The allosteric ligand Org 27569 promotes agonist binding to CB1, yet blocks the agonist-induced conformational changes in TM6. Org 27569 traps the receptor in a distinct agonist-bound, but nonsignaling conformational state. ^[3]

Protocol (from reference)

Kinase Assay:^[2]

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.

Cell Research:^[2]

Cell lines: HEK293
Concentrations: ~10 μM
Incubation Time: 5 to 15 min
Method: Cells expressing CB1 receptors are exposed to ORG27569 (10 μM) for 5 to 15 min. For toxin treatment to abrogate Gi coupling effects, PTX is added to the medium at 5 ng/ml. Following an 18-h incubation in the presence of toxin, cells are washed twice with PBS and treated with compounds. Cells are washed with ice-cold PBS, and cell lysates are obtained by harvesting the cells with ice-cold lysis buffer (150 mM NaCl, 1.0% IGEPAL CA-630, 0.5% sodium deoxycholate, 0.1% SDS, and 50 mM Tris, pH 7.5 containing 4-(2-aminoethyl)benzenesulfonyl fluoride, pepstatin A, E-64, bestatin, leupeptin, and aprotinin as protease inhibitors).

References

Solubility (25°C)

In vitro	DMSO	82 mg/mL (200.02 mM)
	Water	Insoluble
	Ethanol	Insoluble

Chemical Information

Molecular Weight	409.95
Formula	C₂₄H₂₈ClN₃O
CAS No.	868273-06-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4

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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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