Cas No.: | 460330-27-2 |
Chemical Name: | 3-((4-Cyclohexylpiperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6-methoxyquinolin-2(1H)-one |
Synonyms: | GT 949 |
SMILES: | O=C1NC2=C(C=C(OC)C=C2)C=C1C(N3CCN(C4CCCCC4)CC3)C5=NN=NN5CCC6=CC=CC=C6 |
Formula: | C30N7O2H37 |
M.Wt: | 527.6605 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM[1]. |
Target: | EC50: 0.26±0.03 nM (EAAT2)[1] |
In Vitro: | 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]. |
References: | [1]. Kortagere S, et al. Identification of Novel Allosteric Modulators of Glutamate Transporter EAAT2. ACS Chem Neurosci. 2018 Mar 21;9(3):522-534. |