MRK 016

Key Product Details

Product Description

MRK 016 is a GABA_A receptor inverse agonist selective for the α5-subtype (EC₅₀ = 3 nM). Exhibits affinity at benzodiazepine binding site of recombinant human GABA_A receptors (K_i 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 for MRK 016

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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.

Select a batch to recalculate based on the batch molecular weight:

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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

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 8 publications citing the usage of this 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 GABA_A 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 GABA_A α5 receptors with cognition enhancing properties. J.Med.Chem. 2004 PMID: 15537339

Product Documents for MRK 016