Biological Activity
High affinity and selective CB1 antagonist (Ki = 3.3 nM). Exhibits >100-fold selectivity for CB1 over CB2 receptors. Improves glucose homeostasis, reverses hepatic steatosis and reduces body weight in diet-induced obese mice. Orally available and non-brain penetrant.
Technical Data
| M. Wt | 556.46 |
| Formula | C26H23Cl2N5O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1245626-05-4 |
| PubChem ID | 46912919 |
| InChI Key | XBHQLFVDGLPBCK-UHFFFAOYSA-N |
| Smiles | O=C(NN3CCS(CC3)(=O)=O)C1=NN(C2=CC=C(Cl)C=C2Cl)C(C4=CC=C(C#CCCC#N)C=C4)=C1C |
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 | 11.13 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 556.46. 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 | 1.8 mL | 8.99 mL | 17.97 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.59 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Tam et al (2010) Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity. J.Clin.Invest. 120 2953 PMID: 20664173
Bowles et al (2015) A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome. Proc.Natl.Acad.Sci.U.S.A. 112 285 PMID: 25535367
Keywords: AM 6545, supplier, AM6545, CB1, receptors, antagonists, high, affinity, selective, obesity, lipids, glucose, CB1, Receptors, CB1, Receptors, Tocris Bioscience
