For research use only. Not for therapeutic Use.
GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM[1].
GT 949 (GT949) enhances glutamate transport with an EC50 of 0.26 ± 0.03 nM. GT 949 also demonstrates selectivity to EAAT2 and has no effect on glutamate activity mediated by EAAT1 or EAAT3[1].
GT 949 is also tested for its effect on glutamate uptake kinetics in EAAT2-transfected cells. GT 949 enhances glutamate transport in a noncompetitive fashion, with increase in Vmax of about 47%[1].
Catalog Number | I019592 |
CAS Number | 460330-27-2 |
Synonyms | 3-[(4-cyclohexylpiperazin-1-yl)-[1-(2-phenylethyl)tetrazol-5-yl]methyl]-6-methoxy-1H-quinolin-2-one |
Molecular Formula | C30H37N7O2 |
Purity | ≥95% |
InChI | InChI=1S/C30H37N7O2/c1-39-25-12-13-27-23(20-25)21-26(30(38)31-27)28(36-18-16-35(17-19-36)24-10-6-3-7-11-24)29-32-33-34-37(29)15-14-22-8-4-2-5-9-22/h2,4-5,8-9,12-13,20-21,24,28H,3,6-7,10-11,14-19H2,1H3,(H,31,38) |
InChIKey | ZVWPOIUAPXDLMB-UHFFFAOYSA-N |
SMILES | COC1=CC2=C(C=C1)NC(=O)C(=C2)C(C3=NN=NN3CCC4=CC=CC=C4)N5CCN(CC5)C6CCCCC6 |
Reference | [1]. Kortagere S, et al. Identification of Novel Allosteric Modulators of Glutamate Transporter EAAT2. ACS Chem Neurosci. 2018 Mar 21;9(3):522-534. |