Biological Activity
GABAA receptor inverse agonist selective for the α5-subtype (EC50 = 3 nM). Exhibits affinity at benzodiazepine binding site of recombinant human GABAA receptors (Ki values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α3-, α1-, α2-, and α5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity.
Licensing Information
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Compound Libraries
MRK 016 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 368.39 |
| Formula | C17H20N8O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 342652-67-9 |
| PubChem ID | 6918583 |
| InChI Key | QYSYOGCIDRANAR-UHFFFAOYSA-N |
| Smiles | CC(C)(C)C2=C1C=NN=C(C4=NOC(C)=C4)N1N=C2OCC3=NC=NN3C |
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 | 36.84 | 100 | |
| ethanol | 3.68 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 368.39. 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 | 2.71 mL | 13.57 mL | 27.15 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.43 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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References
References are publications that support the products' biological activity.
Chambers et al (2004) An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing properties. J.Med.Chem. 47 5829 PMID: 15537339
Atack et al (2009) In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor α5 subtype-selective inverse agonist. J.Pharmacol.Exp.Ther. 331 470 PMID: 19704033
Keywords: MRK 016, supplier, MRK016, GABA, a5, inverse, agonist, alpha5, GABAA, α5, merck, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
