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Org 27569

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Purity:100%

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COA HPLC HNMR

Org 27569

Catalog No. T2635Cas No. 868273-06-7

Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and enhanced agonist affinity.

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Pack Size	Price	Availability
2 mg	$31	In Stock
5 mg	$48	In Stock
10 mg	$81	In Stock
25 mg	$159	In Stock
50 mg	$297	In Stock
100 mg	$443	In Stock
1 mL x 10 mM (in DMSO)	$48	In Stock

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Product Introduction

Bioactivity

Description	Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and enhanced agonist affinity.
In vivo	ORG 27569 (3.2 and 5.6 mg/kg, intraperitoneally) significantly reduces both cue-induced and priming-induced reinstatement of cocaine and methamphetamine in rats[4]. At a dosage of 30 mg/kg, intraperitoneally, Org27569 induces appetite suppression independent of CB1 receptors and does not alter the discriminative stimulus effects of anandamide (AEA). Furthermore, an intracerebroventricular administration of Org27569 (100 μg) does not influence the pharmacological effects of CP55,940 administered systemically when compared to a vehicle[5].
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.
Cell Research	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).(Only for Reference)

Chemical Properties

Molecular Weight	409.95
Formula	C24H28ClN3O
Cas No.	868273-06-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41 mg/mL (100 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4393 mL	12.1966 mL	24.3932 mL	121.9661 mL
5 mM	0.4879 mL	2.4393 mL	4.8786 mL	24.3932 mL
10 mM	0.2439 mL	1.2197 mL	2.4393 mL	12.1966 mL
20 mM	0.1220 mL	0.6098 mL	1.2197 mL	6.0983 mL
50 mM	0.0488 mL	0.2439 mL	0.4879 mL	2.4393 mL
100 mM	0.0244 mL	0.1220 mL	0.2439 mL	1.2197 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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