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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.
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)
MRK 016 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 will 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|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for MRK 016, please let us know.
Keywords: MRK 016, MRK 016 supplier, MRK016, GABA, a5, inverse, agonist, alpha5, GABAA, α5, merck, Receptors, 3817, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for MRK 016 include:
Zanos et al (2017) A Negative Allosteric Modulator for α5 Subunit-Containing GABA Receptors Exerts a Rapid and Persistent Antidepressant-Like Action without the Side Effects of the NMDA Receptor Antagonist KA in Mice. Eneuro 4 PMID: 28275719
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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