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)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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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
Juneet 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