Rimonabant
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Rimonabant(SR141716)是一种强效的中央大麻素受体(CB1)选择性拮抗剂,对CB1和CB2受体的Ki值分别为1.8 nM和514 nM[1]。
Rimonabant (SR141716)对CB1的选择性是CB2的285倍(CB1的Ki = 1.8 nM,CB2的Ki = 514 nM)。Rimonabant对CB1-Rs的亲和力比CB2-Rs高50倍,对CB1-Rs的Ki值为6.18 nM[1]。 此外,单独服用Rimonabant可改变摄食行为。而且,Rimonabant已被报道可选择性地减少可口食物和饮料的消耗。也有报道,在对食物消耗的影响不大的时候,Rimonabant可降低大鼠对蔗糖的摄入、小鼠对酒精的消耗和狨猴对甜食的摄入[2]。
参考文献:
[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.
- 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
Storage | Store at -20°C |
M.Wt | 463.79 |
Cas No. | 168273-06-1 |
Formula | C22H21Cl3N4O |
Solubility | ≥23.19 mg/mL in DMSO; insoluble in H2O; ≥57.1 mg/mL in EtOH |
Chemical Name | 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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 |
质量控制和MSDS
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