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MRK-016

Chemical Structure : MRK-016

CAS No.: 342652-67-9

MRK-016 (MRK016;MRK 016)

Catalog No.: PC-42117Not For Human Use, Lab Use Only.

MRK-016 (MRK016) is a potent, functionally selective, CNS-penetrating and orally bioavailable inverse agonist of benzodiazepine site of GABAA α5 receptor with Ki of 0.8-1.5 nM for α1-, α2-, α3-, and α5-containing GABAA receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MRK-016 (MRK016) is a potent, functionally selective, CNS-penetrating and orally bioavailable inverse agonist of benzodiazepine site of GABAA α5 receptor with Ki of 0.8-1.5 nM for α1-, α2-, α3-, and α5-containing GABAA receptors.
MRK-016 has inverse agonist efficacy selective for the α5 subtype, increases long-term potentiation in mouse hippocampal slices.
MRK-016 enhances performance in animal models of cognition, does not exhibit the convulsant, proconvulsant, or anxiogenic activity associated with nonselective GABAA inverse agonists.

Physicochemical Properties

M.Wt 368.3931
Formula C17H20N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Pyrazolo[1,5-d][1,2,4]triazine, 3-(1,1-dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-

References

1. Chambers MS, et al. J Med Chem. 2004 Nov 18;47(24):5829-32.

2. Jones P, et al. Bioorg Med Chem Lett. 2006 Feb 15;16(4):872-5.

3. Atack JR, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84.

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