Biological Activity
Benzodiazepine inverse agonist. Binds with high affinity to both diazepam-sensitive (DS) and diazepam-insensitive (DI) GABAA receptors (Ki values are ~ 0.2 and ~ 2.6 nM for DS and DI receptors respectively). Antagonizes effects of ethanol on locomotor behavior and suppresses ethanol intake in alcohol-preferring rats.
Compound Libraries
Ro 19-4603 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 319.38 |
| Formula | C15H17N3O3S |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 99632-94-7 |
| PubChem ID | 127382 |
| InChI Key | ZIGMMUKDYCABPW-UHFFFAOYSA-N |
| Smiles | CN1CC2=C(N=CN2C2=C(SC=C2)C1=O)C(=O)OC(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 | 31.94 | 100 | |
| ethanol | 31.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 319.38. 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 | 3.13 mL | 15.66 mL | 31.31 mL |
| 5 mM | 0.63 mL | 3.13 mL | 6.26 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.13 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wong and Skolnick (1992) High affinity ligands for 'diazepam-insensitive' benzodiazepine receptors. Eur.J.Pharmacol. 225 63 PMID: 1311690
June et al (1995) Effects of the benzodiazepine inverse agonist RO19-4603 on the maintenance of tolerance to a single dose of ethanol. J.Pharmacol.Exp.Ther. 274 1105 PMID: 7562476
June et al (1998) The novel benzodiazepine inverse agonist RO19-4603 antagonises ethanol motivated behaviours: neuropharmacological studies. Brain Res. 784 256 PMID: 9518641
Keywords: Ro 19-4603, supplier, Benzodiazepine, inverse, agonists, GABAA, Receptors, Ro19-4603, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
