MRK 016

Catalog # Availability Size / Price Qty
3817/10
3817/50
MRK 016 | CAS No. 342652-67-9 | GABA-A Receptor Inverse Agonists
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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%

Product Details
Citations (1)
Reviews

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.

Technical Data

M.Wt:
368.39
Formula:
C17H20N8O2
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
342652-67-9

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.

Additional Information

Licensing Caveats:
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)

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Citation for MRK 016

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