MRK 016

• Supplier: Tocris Bioscience
• Catalog: 4041
• Prices: $199.00, $825.00
• Sizes: 10 mg, 50 mg
• Function Type: Agonist
• Cas Number: 783331-24-8
• 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
• Formula: C17H20N8O2
• Molecular Weight: 368.39
• Purity: >98 %
• Description: GABA A receptor inverse agonist selective for the α 5-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 α 3-, α 1-, α 2-, and α 5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity.

Product References

An orally bioavailable, functionally selective inverse agonist at the - An orally bioavailable, functionally selective inverse agonist at the

Chambers MS, Atack JR, Carling RW, Collinson N, Cook SM, Dawson GR, Ferris P, Hobbs SC, O'connor D, Marshall G, Rycroft W, Macleod AM. J Med Chem. 2004 Nov 18;47(24):5829-32.

In vitro and in vivo properties of - In vitro and in vivo properties of

Atack JR, Maubach KA, Wafford KA, O'Connor D, Rodrigues AD, Evans DC, Tattersall FD, Chambers MS, MacLeod AM, Eng WS, Ryan C, Hostetler E, Sanabria SM, Gibson RE, Krause S, Burns HD, Hargreaves RJ, Agrawal NG, McKernan RM, Murphy MG, Gingrich K, Dawson GR, Musson DG, Petty KJ. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84.