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利莫那班 /Rimonabant {[allProObj[0].p_purity_real_show]}

货号：A471490 同义名： SR141716

Rimonabant is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

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Rimonabant 化学结构 CAS号：168273-06-1
Rimonabant 化学结构
CAS号：168273-06-1
Rimonabant 3D分子结构
CAS号：168273-06-1
Rimonabant 化学结构 CAS号：168273-06-1
Rimonabant 3D分子结构 CAS号：168273-06-1
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Rimonabant 纯度/质量文件 产品仅供科研

货号：A471490 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 CB1 ↓ CB2 ↓ 其他靶点 纯度
Otenabant HCl ++++

hCB1, Ki: 0.7 nM

rCB1, Ki: 2.8 nM

 		98+%
AM251 ✔ 98%
Rimonabant +++

hCB1, IC50: 13.6 nM

 		++

hCB2, IC50: 1.64 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Rimonabant 生物活性

靶点

  • CB2

    hCB2, IC50:1.64 μM

  • CB1

    hCB1, IC50:13.6 nM
描述 Rimonabant demonstrates growth inhibition of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is directly targeted by rimonabant[2]. Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of [35S]GTPgS to human cortical membranes in a concentration-dependent manner, with a -log IC50 of 4.7±0.2 (IC50 = 20 μM) and a maximal inhibition of 48±2%[3].
体内研究

Rimonabant (10 mg/kg by gavage) is administered 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 slows 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 [1].

Rimonabant (20 mg daily) demonstrates a significant reduction in many cardiometabolic risk factors[4].
体外研究

Rimonabant demonstrates growth inhibition of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is directly targeted by rimonabant[2].

Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of [35S]GTPgS to human cortical membranes in a concentration-dependent manner, with a -log IC50 of 4.7±0.2 (IC50 = 20 μM) and a maximal inhibition of 48±2%[3].

Rimonabant 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM 10465552
CHO cells Function assay Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=2.51 nM 14736243
CHOK1 cells Function assay Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12 μM 18243711
CHOK1 cells Function assay Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016 μM 19351113

Rimonabant 动物研究

Dose Mice: 0.3 mg/kg - 10 mg/kg[3] (p.o.), 10 mg/kg - 50 mg/kg[4] (p.o.)
Administration p.o.

Rimonabant 参考文献

[1]Seely KA, Brents LK, Franks LN, Rajasekaran M, Zimmerman SM, Fantegrossi WE, Prather PL. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies. Neuropharmacology. 2012 Oct;63(5):9

[2]Leite, C.E., et al. Rimonabant: An antagonist drug of the endocannabinoid system for the treatment of obesity. Pharmacol Rep 61 217-224 (2009).

[3]Zhang B, et al. Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target. Cell. 2019 Jan 24;176(3):636-648.e13.

[4]Erdozain, A. M. et al. The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor: Evidence from postmortem human brain Biochemical Pharmacology (2012), 83(2), 260-268.

Rimonabant 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.78mL

2.16mL

1.08mL

21.56mL

4.31mL

2.16mL

Rimonabant 技术信息

CAS号168273-06-1
分子式C22H21Cl3N4O
分子量 463.787
别名 SR141716
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 120 mg/mL(258.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 51 mg/mL suspension

Tags: Rimonabant | 168273-06-1 | SR141716 | SR 141716 | SR-141716 | Cannabinoid Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Anti-infection | Cannabinoid Receptor | Bacterial | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Rimonabant 纯度/质量文件 | Rimonabant 亚型比较 | Rimonabant 生物活性 | Rimonabant 细胞研究 | Rimonabant 动物研究 | Rimonabant 参考文献 | Rimonabant 实验方案 | Rimonabant 技术信息

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