Biological Activity
Potent and selective cannabinoid CB1 receptor antagonist (Ki = 1.98 nM). Also acts as an inverse agonist reversing adenylyl cyclase inhibition by WIN 55,212-2 (Cat.No. 1038) (IC50 = 48 nM). Displays no activity at CB2 receptors. Reduces food intake and body weight in orally dosed non-obese Wistar rats.
Technical Data
| M. Wt | 500.25 |
| Formula | C22H21Cl3N4O.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 158681-13-1 |
| PubChem ID | 104849 |
| InChI Key | REOYOKXLUFHOBV-UHFFFAOYSA-N |
| Smiles | O=C(NN4CCCCC4)C1=NN(C3=CC=C(Cl)C=C3Cl)C(C2=CC=C(Cl)C=C2)=C1C.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.02 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 500.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2 mL | 10 mL | 19.99 mL |
| 5 mM | 0.4 mL | 2 mL | 4 mL |
| 10 mM | 0.2 mL | 1 mL | 2 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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References
References are publications that support the products' biological activity.
Janiak et al (2007) Blockade of cannabinoid CB1 receptors improves renal function, metabolic profile, and increased survival of obese Zucker rats. Kidney Int. 72 1345 PMID: 17882151
Rinaldi-Carmona et al (1994) SR 141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett. 350 240 PMID: 8070571
Rinaldi-Carmona et al (1995) Biochemical and pharmacological characterisation of SR 141716A, the first potent and selective brain cannabinoid receptor antagonist. Life Sci. 56 1941 PMID: 7776817
Colombo et al (1998) Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci. 63 113 PMID: 9718088
Keywords: SR 141716A, supplier, SR141716A, rimonabant, cannabinoid, cb1, selective, potent, orally, available, inverse, agonists, antagonists, RIMO, Rimonabant, hydrochloride, CB1, Receptors, CB1, Receptors, Tocris Bioscience
