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Rimonabant

现货
Catalog No.
B1429
CB1 受体拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
25mg
¥ 900.00
现货
100mg
¥ 2,500.00
现货
1g
¥ 15,000.00
现货

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Background

Rimonabant (SR141716) is a potent and selective antagonist of central cannabinoid (CB1) receptor with Ki values of 1.8nM and 514nM for CB1 and CB2, respectively [1].

Rimonabant (SR141716) has shown a 285–fold CB1 selectivity (Ki=1.8nM CB1, 514nM CB2). The affinity of Rimonabant for CB1-Rs is 50-fold higher than for CB2-Rs with a Ki value of 6.18nM for CB1-Rs [1]. In addition, Rimonabant has been revealed to produce changes in ingestive behaviors when treatment alone. Moreover Rimonabant has been reported to selectively reduce the consumption of palatable food and drink. Rimonabant has also been noted to decrease sucrose intake in rat, alcohol consumption in mice and sweet diet intake in marmosets when having little effect on bland food consumption [2].

References:
[1]Soudijn W1, van Wijngaarden I, Ijzerman AP. Structure-activity relationships of inverse agonists for G-protein-coupled receptors. Med Res Rev. 2005 Jul;25(4):398-426.
[2] Ravinet Trillou C1, Arnone M, Delgorge C, Gonalons N, Keane P, Maffrand JP, Soubrie P. Anti-obesity effect of SR141716, a CB1 receptor antagonist, in diet-induced obese mice. Am J Physiol Regul Integr Comp Physiol. 2003 Feb;284(2):R345-53. Epub 2002 Oct 24.

文献引用

1. Michael A Taffe, K. M. et al. "Effects of Δ9-tetrahydrocannabinol (THC) vapor inhalation in Sprague-Dawley and Wistar rats." bioRxiv. 2019 February 05
2. He X, Yang L, et al. "Targeting the Endocannabinoid/CB1 Receptor System For Treating Major Depression Through Antidepressant Activities of Curcumin and Dexanabinol-Loaded Solid Lipid Nanoparticles." Cell Physiol Biochem. 2017 Aug 17;42(6):2281-2294. PMID:28848078
3. Jacques Nguyen, K. Creehan, et al. "Repeated vapor inhalation of Δ9-tetrahydrocannabinol induces tolerance to hypothermia in female rats." biorxiv.2017.August 4

Chemical Properties

StorageStore at -20°C
M.Wt463.79
Cas No.168273-06-1
FormulaC22H21Cl3N4O
Solubility≥23.2mg/mL in DMSO
Chemical Name5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide
SDFDownload SDF
Canonical SMILESCC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

配体结合试验

将人CB1和CB2稳定转染HEK 293细胞并且对其细胞膜进行纯化。0.2-8 μg纯化的细胞膜与0.75 nM [3H] CP55,940和Rimonabant在孵育液(50 mM Tris-HCl,5 mM MgCl2,1 mM EDTA,0.3%BSA,pH 7.4)中孵育。非特异性结合被定义为在1 μM CP55,940存在的反应条件。反应在30℃下,Multiscreen中培育1.5小时。反应通过多重过滤终止,并且用冰预冷的洗涤缓冲液(50mM Tris,pH 7.4,0.25% BSA)清洗4次。过滤器上的放射性结合物通过Topcount测量。IC50定义为抑制50%[3H] CP55,940结合时Rimonabant的浓度,并通过非线性回归计算。

细胞实验 [2, 3]:

细胞系

外周血单核细胞(PBMC);角质形细胞株(C5N细胞)

溶解方法

该化合物在DMSO中的溶解度> 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

患者每日服用rimonabant(20 mg)、持续4周;或0.3–10 μM 处理24 h和48 h

应用

使用Rimonabant处理外周血单核细胞(PBMC)并没有诱导单核细胞、B细胞、总T细胞或T细胞亚群发生显著改变;同时,Rimonabant药物治疗后诱导CD16+、CD3–和/或CD56+ 细胞数量的增加;Rimonabant减少角质形细胞株(C5N细胞)存活并诱导其凋亡。

动物实验 [2]:

动物模型

表达CD-1的雄性小鼠模型

剂量

0.1、0.3和1.0 μmol·cm-2 处理6 h或24 h

应用

Rimonabant显著地减少水肿和白细胞浸润并且显示小鼠的局部抗炎活性。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Chu, C. M., Hung, M. S., Hsieh, M. T., Kuo, C. W., Suja, T. D., Song, J. S., Chiu, H. H., Chao, Y. S. and Shia, K. S. (2008) Bioisosteric replacement of the pyrazole 3-carboxamide moiety of rimonabant. A novel series of oxadiazoles as CB1 cannabinoid receptor antagonists. Org Biomol Chem. 6, 3399-3407

2. Malfitano, A. M., Sosa, S., Laezza, C., De Bortoli, M., Tubaro, A. and Bifulco, M. (2011) Rimonabant reduces keratinocyte viability by induction of apoptosis and exerts topical anti-inflammatory activity in mice. Br J Pharmacol. 162, 84-93

3. Almestrand, S., Wang, X., Jeppsson-Ahlberg, A., Nordgren, M., Flygare, J., Christensson, B., Rossner, S. and Sander, B. (2015) Influence of rimonabant treatment on peripheral blood mononuclear cells; flow cytometry analysis and gene expression profiling. PeerJ. 3, e1056

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Rimonabant

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Rimonabant

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Rimonabant