MRK 016

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Cat.No. 3817 - MRK 016 | C17H20N8O2 | CAS No. 342652-67-9
Description: α5-selective GABAA 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)
Datasheet
Citations (1)
Reviews
Literature

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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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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Keywords: MRK 016, MRK 016 supplier, MRK016, GABA, a5, inverse, agonist, alpha5, GABAA, α5, merck, Receptors, 3817, Tocris Bioscience

1 Citation for MRK 016

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 Ketamine in Mice. Eneuro 4 PMID: 28275719


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