MRK-016
Cat. No.：YN360025
| 产品名称: | MRK-016 |
| CAS No.: | 342652-67-9 |
| 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 |
| Synonyms: | MRK016;MRK 016 |
| 分子量: | 368.39 |
| 分子式: | C₁₇H₂₀N₈O₂ |
| SMILES: | CN1N=CN=C1COC2=NN3C(C4=NOC(C)=C4)=NN=CC3=C2C(C)(C)C |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | MRK-016 是一种选择性的，可口服的，可透过血脑屏障的GABAAα5 receptor拮抗剂，对 GABAAα5 的EC50值为 3 nM，对人 GABAAα1β3γ2，GABAAα2β3γ2，GABAAα3β3γ2 和 GABAAα5β3γ2 的Ki值分别为 0.83，0.85，0.77 和 1.4 nM。 |
| IC50和靶点: | |
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Chambers, M.S., Atack, J.R., Carling, R.W., et al.An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing propertiesJ. Med. Chem.47(24),5829-5832(2004)
Eimerbrink, M.J., Pendry, R.J., Hodges, S.L., et al.The α5-GABAAR inverse agonist MRK-016 upregulates hippocampal BDNF expression and prevents cognitive deficits in LPS-treated mice, despite elevations in hippocampal AβBehav. Brain Res.359,871-877(2019)
Zanos, P., Nelson, M.E., Highland, J.N., et al.A negative allosteric modulator for α5 subunit-containing GABA receptors exerts a rapid and persistent antidepressant-like action without the side effects of the nmda receptor antagonist ketamine in miceeNeuro4(1),e0285-0216.2017(2017)
