盐酸利莫那班

概述生物活性靶点体外研究体内研究盐酸利莫那班试剂级价格

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

盐酸利莫那班化学性质

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)

安全信息

危险品标志 :T,Xi
危险类别码 :25-36
安全说明 :26-45
危险品运输编号 :UN 2811 6.1 / PGIII
WGK Germany :3

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)
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.