Rimonabant

Catalog No.S3021

Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane.

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Rimonabant Chemical Structure

Rimonabant Chemical Structure
Molecular Weight: 463.79

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane.
Targets hCB1 hCB2 Acuyl coenzyme A:cholesterol acyltransferase (ACAT
IC50 13.6 nM 1.64 μM [1] 1.5-2.9 μM [2]
In vitro Rimonabant dose-dependently reduces ACAT activity in Raw264.7macrophages with IC50 of 2.9 μM and isolated peritoneal macrophages. Rimonabant inhibits ACATactivity in intact CHO-ACAT1 and CHO-ACAT2 cells and in cell-free assays with approximately equal efficiency with IC50 of 1.5 μM and 2.2 μM for CHO-ACAT1 and CHO-ACAT2, respectively. Consistent with ACAT inhibition, Rimonabant treatment blocks ACAT dependent processes in macrophages, oxysterol-induced apoptosis and acetylated-LDL induced foam cell formation. [2] Rimonabant antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes in a concentration-dependent manner. [3] Rimonabant significantly reduces cell growth and induces cell death of human colorectal cancer cells (DLD-1, CaCo-2 and SW620). Rimonabant is able to alter cell cycle distribution in all the cell lines tested. Particularly, Rimonabant produces a G2/M cell cycle arrest in DLD-1 cells without inducing apoptosis or necrosis. [4]
In vivo Rimonabant is administered intraperitoneally or orally potently and dose-dependently antagonize classical pharmacological and behavioural effectos of cannabinoid receptor agonists. [3] In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer. [4] Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) and MCP-1 (monocyte chemotactic protein-1) serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant. Platelets from obese rats are more sensitive to thrombin-induced aggregation and adhesion to fibrinogen, which are both attenuated by Rimonabant therapy. [5]
Features Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety.

Protocol(Only for Reference)

Kinase Assay: [1]

Radioligand Binding Assay Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 μg of the purified membrane is incubated with 0.75 nM [3H] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 μM of CP55,940. The reactions are incubated for one and a half hours at 30 °C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [3H] CP55,940 and calculated by non-linear regression.
Eu-GTP Binding Assay The Eu-GTP binding assay is performed using the DELFIA Eu-GTP binding kit based on methods developed by Frang et al., with minor modifications as described in the following: 1-4 μg of purified membrane is incubated with Rimonabant and 20 nM CP55,940 in the assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 100 μg/mL saponin, 5 mMMgCl2, 2 μM GDP, 0.5% BSA) at 30 °C for 60 minutes in acroplates. Following the addition of Eu-GTP and incubation for 30 minutes at 30 °C, the assay is terminated by washing four times with the washing buffer provided in the kit. The fluorescence signal of the Eu-GTP is determined with a Victor 2 multilabel reader. The EC50 of Rimonabant at inhibiting 50% of the CP55,940-stimulated Eu-GTP binding is determined from the dose-response curves using non-linear regression. [2]

Cell Assay: [2]

Cell lines Raw 264.7 cells
Concentrations 0,1,4 μM
Incubation Time 17 hours
Method Raw 264.7 cells (2 × 106 /well) in 12-well plates are rinsed with PBS and refed culture media supplemented with varying amounts of Rimonabant 1 hour prior to supplementation with 7-ketocholesterol (7KC). All wells are adjusted to receive equal amounts of vehicle. Following 16-hour incubation, caspase-3 and caspase 3-like activity are determined using a fluorogenic substrate (Ac-DEVD-AFC) and a spectrofluorometer equipped with a microplate reader.

Animal Study: [3]

Animal Models Male mice and male rats
Dosages 20 ml/kg (mice) and 5 ml/kg (rats)
Administration Rimonabant is administered i.p. (30 minutes) or p.o. (1hour) before the i.v. injection of WIN55212-2.
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
1

References

Chemical Information

Download Rimonabant SDF
Molecular Weight (MW) 463.79
Formula

C22H21Cl3N4O

CAS No. 168273-06-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms SR141716
Solubility (25°C) * In vitro DMSO 25 mg/mL (53 mM)
Water <1 mg/mL (<1 mM)
Ethanol 2 mg/mL (4 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.46379 4.6379 9.2758 13.9137

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  • Rimonabant

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    Features:Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety.

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