MRK-016 |CAS:342652-67-9 Probechem Biochemicals

Chemical Structure : MRK-016

CAS No.: 342652-67-9

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MRK-016 (MRK016;MRK 016)

货号: 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-, and α5-containing GABAA receptors.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1580	In stock
25 mg	￥2780	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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-, and α5-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.

物理化学性质&存储条件

分子量	368.3931
分子式	C17H20N8O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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]-

参考文献

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.

MRK-016 (MRK016;MRK 016)

生物&药学活性

物理化学性质&存储条件

参考文献

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MRK-016 (MRK016;MRK 016)

生物&药学活性

物理化学性质&存储条件

参考文献

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