MRK 016
Tocris Bioscience, part of Bio-Techne | Catalog # 3817
α5-selective GABAA inverse agonist
Key Product Details
Description
α5-selective GABAA inverse agonist
Product Description
MRK 016 is a 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)Product Specifications
Molecular Weight
368.39
Formula
C17H20N8O2
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
3-(1,1-Dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-pyrazolo[1,5-d][1,2,4]triazine
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.42 | 50 | |
| Ethanol | 7.37 | 20 |
Preparing Stock Solutions
for MRK 016
The following data is based on the product molecular weight 368.39
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.43 mL | 27.15 mL | 54.29 mL |
| 2.5 mM | 1.09 mL | 5.43 mL | 10.86 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.43 mL |
| 25 mM | 0.11 mL | 0.54 mL | 1.09 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Atack 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. 2009 PMID: 19704033
- Chambers An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing properties. J.Med.Chem. 2004 PMID: 15537339
Product Specific Notices for MRK 016
For research use only
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