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Submit ReviewMRK 016
说明： α5-selective GABAA inverse agonist
化学名： 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
纯度： ≥98% (HPLC)
生物活性 for MRK 016
MRK 016 is a GABAA receptor inverse agonist selective for the α5-subtype (EC50 = 3 nM). Exhibits affinity at benzodiazepine binding site of recombinant human GABAA receptors (Ki 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.
许可信息
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
化合物库 for MRK 016
MRK 016 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for MRK 016
| 分子量 | 368.39 |
| 公式 | C17H20N8O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 342652-67-9 |
| PubChem ID | 6918583 |
| InChI Key | QYSYOGCIDRANAR-UHFFFAOYSA-N |
| Smiles | CC(C)(C)C2=C1C=NN=C(C4=NOC(C)=C4)N1N=C2OCC3=NC=NN3C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for MRK 016
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 18.42 | 50 | |
| ethanol | 7.37 | 20 |
制备储备液 for MRK 016
以下数据基于产品分子量 368.39。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.43 mL | 27.15 mL | 54.29 mL |
| 2.5 mM | 1.09 mL | 5.43 mL | 10.86 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.43 mL |
| 25 mM | 0.11 mL | 0.54 mL | 1.09 mL |
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产品说明书 for MRK 016
参考文献 for MRK 016
参考文献是支持产品生物活性的出版物。
Chambers et al (2004) An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing properties. J.Med.Chem. 47 5829 PMID: 15537339
Atack et al (2009) 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. J.Pharmacol.Exp.Ther. 331 470 PMID: 19704033
If you know of a relevant reference for MRK 016, please let us know.
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关键词: MRK 016, MRK 016 supplier, MRK016, GABA, a5, inverse, agonist, alpha5, GABAA, α5, merck, Receptors, 3817, Tocris Bioscience
1 篇 MRK 016 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MRK 016 的部分引用包括：
Zanos et al (2017) 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 KA in Mice. Eneuro 4 PMID: 28275719
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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