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Chemical Structure : MRK-016
CAS No.: 342652-67-9
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-, andα5-containing GABAA receptors.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $144 | In stock | |
| 50 mg | $600 | In stock | |
| 100 mg | Get quote | ||
| 250 mg | Get quote | ||
| 1 g | Get quote |
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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-, andα5-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.
| M.Wt | 368.3931 | |
| Formula | C17H20N8O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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]- |
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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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