Rimonabant HCl

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 However, it was withdrawn because of the severe byproduct in 2009, especially depression and anxiety.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.

溶解方案(细胞实验)

DMSO 中的溶解度 : 33.33 mg/mL (66.63 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: 2.5 mg/mL (5.00 mM); 悬浊液; 超声助溶 此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (5.00 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"