Ro 19-4603

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Cat.No. 1995 - Ro 19-4603 | C15H17N3O3S | CAS No. 99632-94-7
Description: Benzodiazepine inverse agonist
Chemical Name: 5,6-Dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a]thieno[2,3-f][1,4]diazepine-3-carboxylic acid 1,1-dimethylethyl ester
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

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

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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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 31.94 100
DMSO 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 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
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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References

References are publications that support the biological activity of the product.

Wong and Skolnick (1992) High affinity ligands for 'D.pam-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


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Keywords: Ro 19-4603, Ro 19-4603 supplier, Benzodiazepine, inverse, agonists, GABAA, Receptors, Ro19-4603, 1995, Tocris Bioscience

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