MRK 016
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%
Biological Activity
MRK 016 is a GABA A receptor inverse agonist selective for the α5-subtype (EC 50 = 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.Technical Data
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
Background References
-
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing properties.
Chambers et al.
J.Med.Chem., 2004;47:5829 -
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.
Atack et al.
J.Pharmacol.Exp.Ther., 2009;331:470
Product Datasheets
Reconstitution Calculator
Molarity Calculator
Citation for MRK 016
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for MRK 016
There are currently no reviews for this product. Be the first to review MRK 016 and earn rewards!
Have you used MRK 016?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
