计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。
概述
Rimonabant是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。An immunomodulatory CB1 receptor inverse agonist.
Information
Rimonabant (SR141716) is a selective antagonist ofCB1withIC50of 13.6 nM andEC50of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor ofacyl CoA:cholesterol acyltransferases(ACAT) 1 and 2and inhibits mycobacterial MmpL3.
In vitro
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. 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. 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.
In vivo
Rimonabant is administered intraperitoneally or orally potently and dose-dependently antagonize classical pharmacological and behavioural effectos of cannabinoid receptor agonists. In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer. 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.
Cell Data
cell lines：
Concentrations：0,1,4 μM
Incubation Time：17 hours
Powder Purity:≥99%
规格
别名
利莫那班 (SR141716)
英文别名
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
规格或纯度
10mM in DMSO
英文名称
Rimonabant (SR141716)
生化机理
Rimonabant（SR141716）是一种选择性 CB1 拮抗剂，在转染 hCB1 的 HEK 293 膜中的 IC50 为 13.6 nM，EC50 为 17.3 nM。Rimonabant 还是酰基 CoA：胆固醇酰基转移酶（ACAT）1 和 2 的双重抑制剂，并能抑制霉菌 MmpL3。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
大麻素 CB1 受体拮抗剂
名称和识别符
EC号
685-399-5
分子类型
小分子
Isomeric SMILES
CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl
PubChem CID
分子量
463.79
技术文档
高级数据
产品属性
| ALogP | 6.5 |
|---|
关联靶点（人）
CNR1
Tclin
大麻素受体 1(Cannabinoid receptor 1)
(118 活性数据)
CNR2
Tchem
大麻素受体 2(Cannabinoid receptor 2)
(3 活性数据)
CYP2C9
Tchem
细胞色素 P450 2C9(Cytochrome P450 2C9)
(1 活性数据)
KCNH2
Tclin
钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2)
(2 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 69 mg/mL (199.13 mM);
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
常见问题
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 168273-06-1，分子式为 C22H21Cl3N4O，分子量为 463.79 g/mol。
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