Biological Activity
CB2 antagonist/inverse agonist (Ki = 31.2 nM) that displays 165-fold selectivity over CB1 receptors. Behaves as a weak partial/inverse agonist at CB1 receptors.
Technical Data
| M. Wt | 504.37 |
| Formula | C23H25IN2O3 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 164178-33-0 |
| PubChem ID | 4302963 |
| InChI Key | JHOTYHDSLIUKCJ-UHFFFAOYSA-N |
| Smiles | COC1=CC=C(C=C1)C(=O)C1=C(C)N(CCN2CCOCC2)C2=CC(I)=CC=C12 |
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 | 50.44 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 504.37. 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 | 1.98 mL | 9.91 mL | 19.83 mL |
| 5 mM | 0.4 mL | 1.98 mL | 3.97 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.98 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hosohata et al (1997) AM630 is a competitive cannabinoid receptor antagonist in the guinea pig brain. Life Sci. 61 PL115 PMID: 9284087
Hosohata et al (1997) AM630 antagonism of cannabinoid-stimulated [35S]GTPγS binding in the mouse brain. Eur.J.Pharmacol. 321 R1 PMID: 9083796
Landsman et al (1998) AM630 is an inverse agonist at the human cannabinoid CB1 receptor. Life Sci. 62 PL109 PMID: 9496703
Ross et al (1999) Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. Br.J.Pharmacol. 126 665 PMID: 10188977
Keywords: AM 630, supplier, CB2, selective, antagonists, inverse, agonists, Cannabinoids, Receptors, AM630, cb2r, CB2, Receptors, Tocris Bioscience
