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Rimonabant

Rimonabant

产品编号 T1519L   CAS 168273-06-1
别名: SR141716, 利莫那班

Rimonabant (SR141716) 是一种选择性的、能透过血脑屏障的中心大麻素受体 1 拮抗剂, Ki 值为 1.8 nM。它也能够抑制分枝杆菌膜蛋白 3。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 Rimonabant hydrochloride 的水溶性和稳定性通常比游离态更好。

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Rimonabant Chemical Structure
Rimonabant, CAS 168273-06-1
规格 价格/CNY 货期 数量
5 mg ¥ 255 待询
10 mg ¥ 412 待询
25 mg ¥ 828 待询
50 mg ¥ 1,320 待询
100 mg ¥ 1,990 待询
200 mg ¥ 2,990 待询
1 mL * 10 mM (in DMSO) ¥ 451 待询

Rimonabant 的其他形式现货产品:

Rimonabant hydrochloride
其他形式的 Rimonabant:
产品目录号及名称: Rimonabant (T1519L)
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选择批次  
纯度: 99.91%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.
靶点活性 hCB2:1.64 μM, hCB1:13.6 nM
体外活性 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. [2] 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. [3] Rimonabant significantly reduces cell growth and induces cell death of human colorectal cancer cells (DLD-1, CaCo-2 and SW620). Rimonabant is able to alter cell cycle distribution in all the cell lines tested. Particularly, Rimonabant produces a G2/M cell cycle arrest in DLD-1 cells without inducing apoptosis or necrosis. [4]
体内活性 Rimonabant is administered intraperitoneally or orally potently and dose-dependently antagonize classical pharmacological and behavioural effectos of cannabinoid receptor agonists. [3] In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer. [4] 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. [5]
激酶实验 Radioligand Binding Assay: Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 μg of the purified membrane is incubated with 0.75 nM [3H] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 μM of CP55,940. The reactions are incubated for one and a half hours at 30 °C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50 mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [3H] CP55,940 and calculated by non-linear regression.
细胞实验 Raw 264.7 cells (2 × 106 /well) in 12-well plates are rinsed with PBS and refed culture media supplemented with varying amounts of Rimonabant 1 hour prior to supplementation with 7-ketocholesterol (7KC). All wells are adjusted to receive equal amounts of vehicle. Following 16-hour incubation, caspase-3 and caspase 3-like activity are determined using a fluorogenic substrate (Ac-DEVD-AFC) and a spectrofluorometer equipped with a microplate reader. (Only for Reference)
别名 SR141716, 利莫那班
分子量 463.79
分子式 C22H21Cl3N4O
CAS No. 168273-06-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: <1 mg/mL

Ethanol: 2 mg/mL (4.31 mM)

DMSO: 24 mg/mL (51.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.1561 mL 10.7807 mL 21.5615 mL 53.9037 mL
DMSO 5 mM 0.4312 mL 2.1561 mL 4.3123 mL 10.7807 mL
10 mM 0.2156 mL 1.0781 mL 2.1561 mL 5.3904 mL
20 mM 0.1078 mL 0.539 mL 1.0781 mL 2.6952 mL
50 mM 0.0431 mL 0.2156 mL 0.4312 mL 1.0781 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Chu CM, et al, Org Biomol Chem, 2008, 6(18), 3399-3407 2. Netherland C, et al, Biochem Biophys Res Commun, 2010, 398(4), 671-676. 3. Rinaldi-Carmona M, et al, FEBS Lett, 1994, 350(2-3), 240-244. 4. Santoro A, et al, Int J Cancer, 2009, 125(5), 1996-12003. 5. Schafer A, et al, Br J Pharmacol, 2008, 154(5), 1047-1054.

文献引用

1. Li P, Cao S, Huang Y, et al. A novel chemical inhibitor suppresses breast cancer cell growth and metastasis through inhibiting HPIP oncoprotein. Cell Death Discovery. 2021, 7(1): 1-12.
CB2R agonist 2 ML-193 CB2R agonist 3 ML-184 TM38837 CB1-IN-1 Hemopressin(human, mouse) TFA AM-2232

相关化合物库

该产品包含在如下化合物库中:
抗感染化合物库 抗阿尔茨海默症化合物库 ReFRAME 相关化合物库 表型筛选靶点鉴定库 口服活性化合物库 NO PAINS 化合物库 上市药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Rimonabant 168273-06-1 GPCR/G Protein Metabolism Microbiology/Virology Cannabinoid Receptor Antibacterial Acyltransferase SR-141716 SR 141716 Inhibitor SR141716 inhibit 利莫那班 Bacterial inhibitor

 

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