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Submit ReviewAVE 1625
Description: Potent and selective CB1 receptor antagonist
Alternative Names: Drinabant
Chemical Name: N-[1-[Bis(4-chlorophenyl)methyl]-3-azetidinyl]-N-(3,5-difluorophenyl)methanesulfonamide
Purity: ≥98% (HPLC)
Biological Activity
Potent and selective CB1 receptor antagonist (IC50 values are 25 and 10 nM for human and rat CB1R, respectively). Exhibits >400-fold selectivity for CB1 over CB2 receptors. Attenuates Olanzapine (Cat. No. 4349) induced weight gain and food intake in rats with no effect on energy expenditure or motility. Also improves cognitive function in rodent schizophrenia models and ameliorates extrapyramidal side-effects of antipsychotics.
Technical Data
| M. Wt | 497.38 |
| Formula | C23H20Cl2F2N2O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 358970-97-5 |
| PubChem ID | 10278470 |
| InChI Key | IQQBRKLVEALROM-UHFFFAOYSA-N |
| Smiles | CS(=O)(N(C1=CC(F)=CC(F)=C1)C2CN(C(C3=CC=C(C=C3)Cl)C4=CC=C(C=C4)Cl)C2)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.74 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 497.38. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.01 mL | 10.05 mL | 20.11 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.02 mL |
| 10 mM | 0.2 mL | 1.01 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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References
References are publications that support the biological activity of the product.
Herling et al (2007) CB1 receptor antagonist AVE1625 affects primarily metabolic parameters independently of reduced food intake in Wistar rats. Am.J.Physiol.Endocrinol.Metab. 293 E826 PMID: 17595216
Liebig et al (2010) Profiling of energy metabolism in olanzapine-induced weight gain in rats and its prevention by the CB1-antagonist AVE1625. Obesity 18 1952 PMID: 20168311
Black et al (2011) AVE1625, a cannabinoid CB1 receptor antagonist, as a co-treatment with antipsychotics for schizophrenia: improvement in cognitive function and reduction of antipsychotic-side effects in rodents. Psychopharmacology (Berl.) 215 149 PMID: 21181124
If you know of a relevant reference for AVE 1625, please let us know.
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Keywords: AVE 1625, AVE 1625 supplier, AVE1625, cannabinoid, receptor, antagonist, potent, selective, CB1, CB1R, anti-obesity, Drinabant, Receptors, 6763, Tocris Bioscience
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