Rimonabant (Synonyms: SR141716) |
رقم الكتالوجGC17259
One-Click Copy Product Info
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ريمونابانت (SR141716) هو مضاد لمستقبلات القنب المركزي (CB1) قوي للغاية ، مخترق في الدماغ وانتقائي مع Ki 1.8 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 168273-06-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Kinase experiment [1]: | |
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Radioligand Binding Assay |
Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 μg of the purified membrane is incubated with 0.75 nM [3H] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 μM of CP55,940. The reactions are incubated for one and a half hours at 30 °C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [3H] CP55,940 and calculated by non-linear regression. |
| Cell experiment [2, 3]: | |
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Cell lines |
Peripheral blood mononuclear cells (PBMC); keratinocyte cell line (C5N cells) |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
Patients received rimonabant 20 mg daily, for 4 weeks; or 0.3–10 μM for 24 h and 48 h |
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Applications |
Treatment with rimonabant in peripheral blood mononuclear cells (PBMC) did not induce significant changes of monocytes, B cells, total T cells or T cell subsets. Moreover, there was a small but significant increase in CD16+, CD3–, and/or CD56+ cells after rimonabant therapy. Additionally, Rimonabant reduced keratinocyte cell line (C5N cells) viability by induction of apoptosis. |
| Animal experiment [2]: | |
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Animal models |
Male CD-1 mice model |
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Dosage form |
0.1,0.3, and 1.0μmol·cm-2 for 6 h or 24 h |
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Applications |
Rimonabant significantly reduced oedema and leukocyte infiltrate, and showed topical anti-inflammatory activity in mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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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| Cas No. | 168273-06-1 | SDF | |
| المرادفات | SR141716 | ||
| Chemical Name | 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide | ||
| Canonical SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl | ||
| Formula | C22H21Cl3N4O | M.Wt | 463.79 |
| الذوبان | ≥ 23.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1561 mL | 10.7807 mL | 21.5615 mL |
| 5 mM | 431.2 μL | 2.1561 mL | 4.3123 mL |
| 10 mM | 215.6 μL | 1.0781 mL | 2.1561 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)