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/ 大麻素受体 / Rimonabant/利莫那班

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

货号：A471490 同义名： SR141716

Rimonabant是一种选择性的中枢大麻素CB1受体拮抗剂，Ki值为1.8 nM。

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Type HazMat fee for 500 gram (Estimated)
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Rimonabant/利莫那班 化学结构 CAS号：168273-06-1
Rimonabant/利莫那班 化学结构
CAS号：168273-06-1
Rimonabant/利莫那班 3D分子结构
CAS号：168273-06-1
Rimonabant/利莫那班 化学结构 CAS号：168273-06-1
Rimonabant/利莫那班 3D分子结构 CAS号：168273-06-1
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Rimonabant/利莫那班 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

 		99%
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/利莫那班 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/利莫那班 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 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/利莫那班 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/利莫那班 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/利莫那班 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/利莫那班 技术信息

CAS号168273-06-1
分子式C22H21Cl3N4O
分子量 463.79
SMILES Code C4=C([N]2N=C(C(NN1CCCCC1)=O)C(=C2C3=CC=C(Cl)C=C3)C)C(=CC(=C4)Cl)Cl
MDL No. MFCD04034714
别名 SR141716
运输蓝冰
InChI Key JZCPYUJPEARBJL-UHFFFAOYSA-N
Pubchem ID 104850
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
溶解方案

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/利莫那班 纯度/质量文件 | Rimonabant/利莫那班 亚型比较 | Rimonabant/利莫那班 生物活性 | Rimonabant/利莫那班 细胞研究 | Rimonabant/利莫那班 动物研究 | Rimonabant/利莫那班 参考文献 | Rimonabant/利莫那班 实验方案 | Rimonabant/利莫那班 技术信息

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