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CAS No.: 158681-13-1

Rimonabant HCl/盐酸利莫那班 Catalog No. CSN10030

Synonyms: SR 141716A Hydrochloride;SR 141716A;Rimonabant free base

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

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技术信息

生物活性

描述Rimonabant HCl is a hydrochloride form of Rimonabant. Rimonabant is a first selective oral antagonist of CB1 (cannabinoid receptor 1), which belongs to the guanine-nucleotide-binding protein (G-protein) coupled receptor family. In CB1 transfected HEK293 cells, the IC50 concentration of rimonabant was 13.6 nM and the EC50 concentration was 17.3 nM. Rimonabant was famous for its potent anorectic anti-obesity ability for decades and has been demonstrated to effectively reduce body weight by inducing a reduction in appetite. It also benefits for lowing cardiovascular metabolic risk events. However, it was withdrawn because of the severe byproduct in 2009, especially depression and anxiety. Mechanically, rimonabant promotes adenylate cyclase activity in a dose-dependent, stereoselective and pertussis toxin-sensitive manner by directly targeting to CB1. In vitro, rimonabant dose-dependently reduced ACAT activity in Raw264.7 macrophages and isolated peritoneal macrophages with an IC50 of 2.9 μM. Rimonabant also inhibited ACAT activity in CHO-ACAT1 and CHO-ACAT2 cells with an IC50 of 1.5 μM and 2.2 μM respectively. Rimonabant treatment blocks ACAT-related processes in macrophages, including oxysterol-induced apoptosis, and acetylated LDL-induced foam cell formation. Rimonabant was able to alter the cell cycle distribution in almost all type of cell lines and then significantly reduces cell growth and induces death in human colorectal cancer cells (DLD-1, CaCo-2 and SW620). However, rimonabant causes cell cycle arrest in DLD-1 cells without inducing apoptosis or necrosis. In vivo, Rimonabant significantly reduced the formation of abnormal crypt foci (ACF) before colorectal cancer formation in the oxidative azomethane-induced colon cancer model. In the experiment of long-term rimonabant treated obese Zucker rats, platelet-bound fibrinogen, serum levels of RANTES (normal T cell expression and secretion of regulatory proteins) and MCP-1 (monocyte chemoattractant protein-1) were decreased to the levels observed in lean Zucker rats.
参考文献

[1] Esposito I, Proto MC, et al. The cannabinoid CB1 receptor antagonist rimonabant stimulates 2-deoxyglucose uptake in skeletal muscle cells by regulating the expression of phosphatidylinositol-3-kinase. Mol Pharmacol. 2008 Dec;74(6):1678-86.
[2] Molecule of the month. Rimonabant hydrochloride. Drug News Perspect. 2004 Jul-Aug;17(6):403.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9990 mL
- 9.9950 mL
- 19.9901 mL
- 5 mM
- 0.3998 mL
- 1.9990 mL
- 3.9980 mL
- 10 mM
- 0.1999 mL
- 0.9995 mL
- 1.9990 mL

技术信息

CAS号

158681-13-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H22Cl4N4O

运输

蓝冰

分子量

500.25

别名

SR 141716A Hydrochloride;SR 141716A;Rimonabant free base;SR-141716;A-281;Rimonabant;Acomplia;Zimulti;盐酸利莫那班

溶解度

DMSO	230.0 mg/mL (459.8 mM)
Water	insoluble

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