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GT949

Chemical Structure : GT949

CAS No.: 460330-27-2

GT949 (GT-949)

Catalog No.: PC-49855Not For Human Use, Lab Use Only.

GT949 (GT-949) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.26 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

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Biological Activity

GT949 (GT-949) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.26 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.
GT949 demonstrats high potency to EAAT2 in the in vitro glutamate uptake assays in primary astrocytes with EC50 of 1 nM.
GT949 displays high selectivity to EAAT2 in comparison to other EAATs and did not have any functional effects on NMDA-mediated calcium response.
GT949 is a noncompetitive positive allosteric stimulator of EAAT2, specifically stimulates EAAT2-mediated transport and does not alter EAAT1- and EAAT3-mediated transport.

Physicochemical Properties

M.Wt 527.67
Formula C30H37N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-((4-cyclohexylpiperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6-methoxyquinolin-2(1H)-one

References

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.

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