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MRK-016 {[allProObj[0].p_purity_real_show]}

货号:A899895

MRK-016是一种功能选择性的GABAA α5受体苯二氮平位点的反向激动剂。

MRK-016 化学结构 CAS号:342652-67-9
MRK-016 化学结构
CAS号:342652-67-9
MRK-016 3D分子结构
CAS号:342652-67-9
MRK-016 化学结构 CAS号:342652-67-9
MRK-016 3D分子结构 CAS号:342652-67-9
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MRK-016 纯度/质量文件 产品仅供科研

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产品名称 GABA receptor GABAA receptor 其他靶点 纯度
Niflumic Acid 98%
Ginkgolide A ++

GABA receptor, Ki: 14.5 μM

98%
Valproic acid sodium Autophagy,HDAC 97%
Flumazenil 95%
Bemegride 98%
Bicuculline +++

GABAA receptor, IC50: 2 μM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

MRK-016 生物活性

描述 MRK-016 is a pyrazolotriazine with an affinity of between 0.8 and 1.5 nM for the benzodiazepine binding site of native rat brain and recombinant human alpha1-, alpha2-, alpha3-, and alpha5-containing GABA(A) receptors. It has inverse agonist efficacy selective for the alpha5 subtype. MRK-016 gave good receptor occupancy after oral dosing in rats, with the dose required to produce 50% occupancy being 0.39 mg/kg and a corresponding rat plasma EC(50) value of 15 ng/ml that was similar to the rhesus monkey plasma EC(50) value of 21 ng/ml obtained using [(11)C]flumazenil positron emission tomography. In normal rats, MRK-016 enhanced cognitive performance in the delayed matching-to-position version of the Morris water maze but was not anxiogenic, and in mice it was not proconvulsant and did not produce kindling. MRK-016 had a short half-life in rat, dog, and rhesus monkey (0.3-0.5 h) but had a much lower rate of turnover in human compared with rat, dog, or rhesus monkey hepatocytes[3]. MRK (MRK-016) can prevent LPS- induced cognitive deficits associated with elevated Aβ, and restore hippocampal BDNF expression[4].

MRK-016 参考文献

[1]Eimerbrink MJ, White JD, et al. Administration of the inverse benzodiazepine agonist MRK-016 rescues acquisition and memory consolidation following peripheral administration of bacterial endotoxin. Behav Brain Res. 2015 Jul 15;288:50-3.

[2]Atack JR, Maubach KA, et al. 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 alpha5 subtype-selective inverse agonist. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84.

[3]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. 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 alpha5 subtype-selective inverse agonist. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84

[4]Eimerbrink MJ, Pendry RJ, Hodges SL, Wiles JD, Peterman JL, White JD, Hayes HB, Chumley MJ, Boehm GW. The α5-GABAAR inverse agonist MRK-016 upregulates hippocampal BDNF expression and prevents cognitive deficits in LPS-treated mice, despite elevations in hippocampal Aβ. Behav Brain Res. 2019 Feb 1;359:871-877

MRK-016 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL

MRK-016 技术信息

CAS号342652-67-9
分子式C17H20N8O2
分子量 368.393
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

DMSO: 50 mg/mL(135.72 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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