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Rimonabant

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Chemical Structure| 168273-06-1 同义名 : SR141716
CAS号 : 168273-06-1
货号 : A471490
分子式 : C22H21Cl3N4O
纯度 : 98%
分子量 : 463.787
MDL号 : MFCD04034714
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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

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].
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
实验方案
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
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.