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Description: Postiive allosteric modulator of CB2 receptors; active in vivo
Chemical Name: N-[5-Bromo-1-[(4-fluorophenyl)methyl]-1,2-dihydro-4-methyl-2-oxo-3-pyridinyl]cycloheptanecarboxamide
Purity: ≥98% (HPLC)
Biological Activity
CB2 receptor positive allosteric modulator. Enhances CP 55940 (Cat. No. 0949) and 2-Arachidonylglycerol (Cat. No. 1298)-stimulated binding of [35S]GTPγS to CB2 receptors, but has no effect in the absence of agonist. Exhibits antinociceptive effects in an animal model of neuropathic pain.
Technical Data
| M. Wt | 435.33 |
| Formula | C21H24BrFN2O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2244579-87-9 |
| PubChem ID | 137553165 |
| InChI Key | NSGDYZCDUPSTQT-UHFFFAOYSA-N |
| Smiles | CC1=C(C(N(C=C1Br)CC2=CC=C(C=C2)F)=O)NC(C3CCCCCC3)=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 | 8.71 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 435.33. 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 |
|---|---|---|---|
| 0.2 mM | 11.49 mL | 57.43 mL | 114.86 mL |
| 1 mM | 2.3 mL | 11.49 mL | 22.97 mL |
| 2 mM | 1.15 mL | 5.74 mL | 11.49 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.3 mL |
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References
References are publications that support the biological activity of the product.
Gado et al (2019) Identification of the first synthetic allosteric modulator of the CB2 receptors and evidence of its efficacy for neuropathic pain relief. J.Med.Chem. 62 276 PMID: 29990428
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Keywords: Ec2la, Ec2la supplier, CB2, positive, allosteric, modulator, PAM, cannabinoid, neuropathic, pain, Ec21a, Ec2Ia, Receptors, 6832, Tocris Bioscience
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