MRK 016

Name: MRK 016
Brand: Tocris Bioscience
SKU: 3817

Catalog # 3817 | Tocris Bioscience a Bio-Techne Brand

Citations (1)

COA / SDS

α5-selective GABAA inverse agonist

Key Product Details

Description:	α5-selective GABA_A inverse agonist
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
Purity:	≥98% (HPLC)
Molecular Weight:	368.39

View Full Technical Details for MRK 016

Technical Data
Citations (1) / Reviews

Biological Activity for MRK 016

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)

Compound Libraries for MRK 016

MRK 016 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for MRK 016

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for MRK 016

	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 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

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References for MRK 016

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 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

Citations for MRK 016 (1)

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Citations are publications that use Bio-Techne 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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