GT951 | EAAT2 activator | Probechem Biochemicals

Chemical Structure : GT951

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GT951 (GT-951)

货号: PC-49853Not For Human Use, Lab Use Only.

GT951 (GT-951) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

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生物&药学活性

GT951 (GT-951) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.
GT951 demonstrats high potency to EAAT2 in the in vitro glutamate uptake assays in primary astrocytes with EC50 of 0.3 nM.
GT951 displays high selectivity to EAAT2 in comparison to other EAATs and did not have any functional effects on NMDA-mediated calcium response.
GT951 is a noncompetitive positive allosteric stimulator of EAAT2, specifically stimulates EAAT2-mediated transport and does not alter EAAT1- and EAAT3-mediated transport.

物理化学性质&存储条件

分子量	589.62
分子式	C31H30F3N7O2
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	6-methoxy-3-((1-phenethyl-1H-tetrazol-5-yl)(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)methyl)quinolin-2(1H)-one

参考文献

1. Sandhya Kortagere, et al. ACS Chem Neurosci. 2018 Mar 21;9(3):522-534.

2. Sanjay Da, et al. ACS Med Chem Lett. 2022 Sep 19;13(10):1628-1633.

GT951 (GT-951)

生物&药学活性

物理化学性质&存储条件

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GT951 (GT-951)

生物&药学活性

物理化学性质&存储条件

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