| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R408400-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 大麻素 CB1 受体拮抗剂 |
| 产品介绍 |
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. 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 lines： Concentrations：0,1,4 μM Incubation Time：17 hours Powder Purity:≥99% |
| ALogP | 6.5 |
|---|
| 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 | 104850 |
| 分子量 | 463.79 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 69 mg/mL (199.13 mM); |
|---|
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