Rimonabant

Catalog No.S3021 Synonyms: SR141716

Rimonabant Chemical Structure

Molecular Weight(MW): 463.79

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.

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 170 In stock
USD 270 In stock
USD 370 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
Features Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety.
Targets
hCB1 [1] hCB2 [1] ACAT [2]
13.6 nM 1.64 μM 1.5 μM-2.9 μM
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]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: Male mice and male rats
  • Formulation: Rimonabant is dissolved in two drops of Tween 80, diluted in distilled water.
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 25 mg/mL (53.9 mM)
Ethanol 2 mg/mL (4.31 mM)
Water <1 mg/mL
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 Information

Molecular Weight 463.79
Formula

C22H21Cl3N4O

CAS No. 168273-06-1
Storage powder
in solvent
Synonyms SR141716

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00075205 Completed Healthy|Alcohol Drinking National Institute on Alcohol Abuse and Alcoholism (NIAAA)|Sanofi-Synthelabo|National Institutes of Health Clinical Center (CC) December 31, 2003 Phase 2
NCT00754689 Withdrawn Diabetes Mellitus, Type 2 Sanofi September 2008 Phase 3
NCT00750347 Completed Pain University Hospital, Clermont-Ferrand September 2008 Phase 1
NCT00690456 Terminated Diabetes Mellitus, Type 2 Sanofi May 2008 Phase 3
NCT00678483 Terminated Obesity|Weight Loss Sanofi April 2008 Phase 3
NCT00656487 Completed Cannabis Dependence|Cannabis Withdrawal The Scripps Research Institute|National Institute on Drug Abuse (NIDA) April 2008 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID