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Home   »   Product Pathways  »  Cannabinoid Receptor  »  Rimonabant

Products are for research use only. Not for human use. We do not sell to patients.

CS-0645 Rimonabant

(SR 141716;SR141716;SR-141716)
Structure Price and Availability of    Rimonabant
United States
Size Price Stock
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 Distributor In Japan:  フナコシ株式会社    電話番号:81-3-5684-1620   
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Rimonabant  M.Wt:  463.79
Rimonabant  Formula: C22H21Cl3N4O
Rimonabant  Solubility: DMSO 25 mg/mL; Water <1 mg/mL
Rimonabant  Purity: >98%
Rimonabant  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 168273-06-1

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Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM. IC50 Value: 1.8 nM(Ki) Target: CB1 Receptor 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. 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. in vivo: 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.

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