Rimonabant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rimonabant(SR141716) 是一种选择性中枢大麻素 (CB1) 受体反向激动剂，Ki 为 1.8 nM。

Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

Rimonabant could inhibit the growth of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is the direct target of rimonabant.Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of [35S]GTPgS to human cortical membranes in a concentration dependent manner, with a -log IC50 of 4.7±0.2 (IC50 = 20 μM) and a maximal inhibition of 48±2%.

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 and MCP-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 .Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors.

SR141716

GPCR/G Protein

ACAT

ACAT| hCB1| hCB2

Metabolic Disease

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168273-06-1

463.79

C22H21Cl3N4O

>98% (HPLC)

Ethanol: 2 mg/mL (4.31 mM); DMSO: 25 mg/mL (53.9 mM)

CC1=C(N(N=C1C(=O)NN1CCCCC1)C1=C(Cl)C=C(Cl)C=C1)C1=CC=C(Cl)C=C1

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(-20℃)

With Ice Pack

≥ 2 years