Biological Activity
Selective, partial agonist for the benzodiazepine binding site of the GABAA receptor. Potently inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors (IC50 = 1.3 nM) and displays weak affinity for peripheral benzodiazepine (IC50 = 0.68 - 2.25 μM) and GABA binding sites (IC50 > 10000 μM). Displays anxiolytic activity in vivo following oral administration. .
Compound Libraries
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Technical Data
M. Wt | 309.36 |
Formula | C18H19N3O2 |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 111205-55-1 |
PubChem ID | 163844 |
InChI Key | UBLXQFIFWUEVGJ-UHFFFAOYSA-N |
Smiles | COC1=CC=C(C=C1)N1N=C2C(=CNC3=C2CCCCC3)C1=O |
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 | 30.94 | 100 | |
ethanol | 7.73 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 309.36. 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 | 3.23 mL | 16.16 mL | 32.32 mL |
5 mM | 0.65 mL | 3.23 mL | 6.46 mL |
10 mM | 0.32 mL | 1.62 mL | 3.23 mL |
50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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References
References are publications that support the products' biological activity.
Bennett (1987) Pharmacology of the pyrazolo-type compounds: agonist, antagonist and inverse agonist actions. Physiol.Behav. 41 241 PMID: 2893398
Williams et al (1989) CGS 20625, a novel pyrazolopyridine anxiolytic. J.Pharmacol.Exp.Ther. 248 89 PMID: 2563294
Jarvis et al (1990) CGS 20625, a novel pyrazolopyridine with selective anxiolytic activity. Prog.Clin.Biol.Res. 361 477 PMID: 1981266
Keywords: CGS 20625, supplier, Selective, central, benzodiazepine, receptor, partial, agonists, GABAA, Receptors, CGS20625, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience