| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Rimonabant (also known as SR141716, SR-141716A; A 281) is a novel, potent and selective antagonist (inverse agonist) of cannabinoid CB1 receptor with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is used as an anorectic anti-obesity drug. Its principal impact is appetite suppression. A 285-fold CB1 selectivity has been demonstrated by rimonabant (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. Furthermore, it has been demonstrated that rimonabant, when used as a treatment alone, alters ingestive behaviors.
| Targets |
CB1 ( Ki = 1.8 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Human CB1 and CB2 purify the cell membrane and transfect HEK 293 cells in a stable manner. In the incubation buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3% BSA, pH 7.4), 0.2–8 μg of the purified membrane are incubated with 0.75 nM [3H] CP55,940 and Rimonabant. In the presence of 1 μM of CP55,940, the non-specific binding is defined. The reactions are incubated in Multiscreen at 30 °C for one and a half hours. After four rounds of ice-cold wash buffer (50 mM Tris, pH 7.4, 0.25% BSA), the reactions are stopped by manifold filtration. With Topcount, the radioactivity bound to the filters is measured. The IC50 is computed using non-linear regression and is defined as the concentration of rimonabant needed to inhibit 50% of the binding of [3H] CP55,940.
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| Cell Assay |
Raw 264.7 after rinsing 12-well plates with PBS, cells (2 × 106/well) are refed with culture media supplemented with different amounts of Rimonabant one hour before 7-ketocholesterol (7KC) are added. The amount of vehicle is adjusted so that each well receives the same amount. A fluorogenic substrate (ac-DEVD-AFC) and a spectrofluorometer fitted with a microplate reader are used to measure caspase-3 and caspase 3-like activity after a 16-hour incubation.
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| Animal Protocol |
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| References |
| Molecular Formula |
C22H22CL4N4O
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| Molecular Weight |
500.25
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| Exact Mass |
498.05
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| Elemental Analysis |
C, 52.82; H, 4.43; Cl, 28.35; N, 11.20; O, 3.20
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| CAS # |
158681-13-1
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| Related CAS # |
Rimonabant; 168273-06-1; Rimonabant-d10 hydrochloride; 1044909-61-6
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| Appearance |
Solid powder
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| SMILES |
CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl.Cl
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| InChi Key |
REOYOKXLUFHOBV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21Cl3N4O.ClH/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15;/h5-10,13H,2-4,11-12H2,1H3,(H,27,30);1H
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| Chemical Name |
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9990 mL | 9.9950 mL | 19.9900 mL | |
| 5 mM | 0.3998 mL | 1.9990 mL | 3.9980 mL | |
| 10 mM | 0.1999 mL | 0.9995 mL | 1.9990 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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