盐酸利莫那班
- CAS号:158681-13-1
- 英文名:Rimonabant hydrochloride
- 中文名:盐酸利莫那班
- CBNumber:CB7129375
- 分子式:C22H21Cl3N4O.ClH
- 分子量:500.25
- MOL File:158681-13-1.mol
- 熔点 :230-240°C
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble20mg/mL, clear
- 形态 :powder
- 颜色 :white to beige
- CAS 数据库 :158681-13-1(CAS DataBase Reference)
盐酸利莫那班性质、用途与生产工艺
- 概述 盐酸利莫那班是一种大麻素受体-1(CB1)拈抗剂, 通过阻断脑组织中的大麻素受体来降低人的食欲和烟瘾,可用于肥胖、烟瘾、高血压、血脂异常和2-型糖尿病和代谢综合症的治疗,同时可以降低胆固醇,具有预防肥胖人群患上心脏病和糖尿病的功效,已于2006年在多个国家上市。
- 生物活性 Rimonabant hHydrochloride (SR 141716A Hydrochloride) 是中心大麻素受体 1 (CB1) 高效的、选择性的反向激动剂, Ki 值为1.8 nM。Rimonabant hHydrochloride (SR 141716A Hydrochloride) 也能够抑制分枝杆菌膜蛋白3 (MMPL3)。
-
靶点
CB1
1.8 nM (Ki)
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体外研究
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%. -
体内研究
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.
- 更新日期:2024/11/08
- 产品编号:HY-14137
- 产品名称:Rimonabant Hydrochloride
- CAS编号:
- 包装:1 mg
- 价格:165元
- 更新日期:2024/11/08
- 产品编号:HY-14137
- 产品名称:Rimonabant Hydrochloride
- CAS编号:
- 包装:5 mg
- 价格:331元
- 公司名称:CLEARSYNTH LABS LTD.
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