Biological Activity
Potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors. Also potent GPR55 agonist (EC50 = 39 nM). Also available in a fluorescent form (Cat. No. 2540).
Technical Data
| M. Wt | 555.24 |
| Formula | C22H21Cl2IN4O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 183232-66-8 |
| PubChem ID | 2125 |
| InChI Key | BUZAJRPLUGXRAB-UHFFFAOYSA-N |
| Smiles | CC1=C(N(N=C1C(=O)NN1CCCCC1)C1=C(Cl)C=C(Cl)C=C1)C1=CC=C(I)C=C1 |
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 | 55.52 | 100 | |
| ethanol | 13.88 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 555.24. 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 | 9.01 mL | 18.01 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.6 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
Molarity Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Gatley et al (1996) 125I-labeled AM 251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors. Eur.J.Pharmacol. 307 331 PMID: 8836622
Lan et al (1999) Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J.Med.Chem. 42 769 PMID: 10052983
Pertwee (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 76 1307 PMID: 15670612
Gatley et al (1997) Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors. Life Sci. 61 191 PMID: 9335234
Ryberg et al (2007) The orphan receptor GPR55 is a novel cannabinoid receptor. Br.J.Pharmacol. 152 1092 PMID: 17876302
Keywords: AM 251, supplier, Potent, CB1, antagonist, GPR55, agonist, cannabinoid, receptors, AM251, cb1r, CB1, Receptors, GPR55, CB1, Receptors, Tocris Bioscience
