Rimonabant Inhibitor CAS No. 168273-06-1

Cat. No.	Name	Size	Price
KI0526	Rimonabant	25 mg	$270
	Rimonabant	50 mg	$440
	Rimonabant	100 mg	$592
	Rimonabant	1 g	$4000

Chemical Characteristic

Product Name	Rimonabant
Synonyms	SR-141716, Acomplia
CAS No.	168273-06-1
Molecular Weight	463.79
Formula	C₂₂H₂₁Cl₃N₄O
Chemical Name	5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidinopyrazole-3-carboxamide
Smiles	n1(nc(c(c1c1ccc(cc1)Cl)C)C(=O)NN1CCCCC1)c1c(cc(cc1)Cl)Cl
Chemical Structure

Biological activities

Rimonabant is an antagonist of the cannabinoid receptor type 1 (CB1). Rimonabant has a high affinity for the CB1 with an IC50 of 5 nM. Rimonabant is also shown to be potent in the CHO-hCB1R-Luciferase assay, with an IC50 of 92.5 nM.^[1] Rimonabant has a high affinity for the CB1 with a Ki of 5.6 nM, and low affinity for the CB2 with a Ki > 1 mM. ^[2] Oral treatment of obese (fa/fa) rats with rimonabant (30 mg/kg) daily for 8 weeks abolishes hepatic steatosis. Rimonabant treatment reduces the high plasma level of the proinflammatory cytokine TNFa and increases the reduced plasma level of the anti-inflammatory hormone adiponectin. Rimonabant treatment also improves dyslipidemia by both decreasing plasma levels of triglycerides, free fatty acids, and total cholesterol and increasing the HDLc/LDLc ratio. ^[3] Rimonabant has anti-atherosclerotic effects in LDLR-/- mice. Rimonabant-treated animals have significantly reduced MCP-1, IL12p40/p70, and VCAM-1 levels. ^[4]

Protocols

Rimonabant is dissolved in Tween 80 (1%) and saline (99%).^[5]

References

[1] Lee SH, et al. Pentacycle derivatives as cannabinoid CB1 receptor ligands. Bioorg Med Chem Lett. 2009, 19(23): 6632-6636. [2] Bifulco M, et al. Rimonabant: just an antiobesity drug? Current evidence on its pleiotropic effects. Mol Pharmacol. 2007, 71(6): 1445-1456. [3] Gary-Bobo M, et al. Rimonabant reduces obesity-associated hepatic steatosis and features of metabolic syndrome in obese Zucker fa/fa rats. Hepatology. 2007, 46(1): 122-129. [4] Dol-Gleizes F, et al. Rimonabant, a selective cannabinoid CB1 receptor antagonist, inhibits atherosclerosis in LDL receptor-deficient mice. Arterioscler Thromb Vasc Biol. 2009, 29(1): 12-18. [5] Crespo I, et al. Pretreatment with subeffective doses of Rimonabant attenuates orexigenic actions of orexin A-hypocretin 1. Neuropharmacology. 2008, 54(1): 219-225.

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