盐酸利莫那班
| 中文名称 | 盐酸利莫那班 |
|---|---|
| 中文同义词 | 盐酸利莫那班;5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺盐酸盐;N-(哌啶-1-基)-5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-1H-吡唑-3-甲酰胺盐酸盐;利莫那般;5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺单盐酸盐;利莫那班盐酸盐;利莫那班D10盐酸;盐酸利莫那班[干冰运输] |
| 英文名称 | Rimonabant hydrochloride |
| 英文同义词 | RIMONABANT HYDROCHLORIDE;5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-n-1-piperidinyl-1h-pyrazole-3-carboxamide monohydrochloride;ACOMPLIA;ACOMPLIA (RIMONABANT;RIMONABANT HCL;Rimonabant(Acomplia);RimonabantConsultedStandard;Acomplia, SR141716 |
| CAS号 | 158681-13-1 |
| 分子式 | C22H21Cl3N4O.ClH |
| 分子量 | 500.25 |
| EINECS号 | 233-720-0 |
| 相关类别 | 小分子抑制剂;医药原料;医药原料药;医药、农药及染料中间体;原药中间体;Pharmaceuticals;API;SR141716;Cnbio;Inhibitors;Intermediates & Fine Chemicals;Aromatics;Heterocycles |
| Mol文件 | 158681-13-1.mol |
| 结构式 |  |
盐酸利莫那班 性质
| 熔点 | 230-240°C |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 在DMSO中的溶解度为20mg/mL，澄清 |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| CAS 数据库 | 158681-13-1(CAS DataBase Reference) |
|
CB1 1.8 nM (Ki) |
Rimonabant could inhibit the growth of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is the direct target of rimonabant.
Rimonabant itself (10
-12
-10
-3
M, 12 concentrations) inhibits the basal binding of [
35
S]GTPgS to human cortical membranes in a concentration dependent manner, with a -log IC
50
of 4.7±0.2 (IC
50
= 20 μM) and a maximal inhibition of 48±2%.
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 and MCP-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 .
Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors.