Biological Activity
Positive allosteric modulator of GABAB receptors. Increases the potency and efficacy of GABA at both native and recombinant GABAB receptors (EC50 values are 5.37 and 4.60μM respectively) and enhances the inhibitory effect of the agonist L-baclofen in cultured cortical neurons. Reduces operant self-administration of ethanol in alcohol-preferring rats following i.p. administration.
Compound Libraries
CGP 7930 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 292.46 |
| Formula | C19H32O2 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 57717-80-3 |
| PubChem ID | 5024764 |
| InChI Key | XLWJPQQFJNGUPA-UHFFFAOYSA-N |
| Smiles | CC(C)(CO)CC1=CC(=C(O)C(=C1)C(C)(C)C)C(C)(C)C |
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 | 29.25 | 100 | |
| ethanol | 29.25 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 292.46. 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 | 3.42 mL | 17.1 mL | 34.19 mL |
| 5 mM | 0.68 mL | 3.42 mL | 6.84 mL |
| 10 mM | 0.34 mL | 1.71 mL | 3.42 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Chen et al (2006) Differential modulation by the GABAB receptor allosteric potentiator 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)-phenol (CGP7930) of synaptic transmission in the rat hippocampal CA1 area. J.Pharmacol.Exp.Ther. 317 1170 PMID: 16507713
Liang et al (2006) The GABAB receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 50 632 PMID: 16406445
Urwyler et al (2001) Positive allosteric modulation of native and recombinant γ-aminobutyric acidB receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol.Pharmacol. 60 963 PMID: 11641424
Keywords: CGP 7930, supplier, Positive, modulators, GABAB, receptors, PAM, CGP7930, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience
