Description
GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
Product information
CAS Number: 460330-27-2
Molecular Weight: 527.66
Formula: C30H37N7O2
Chemical Name: 3-[(4-cyclohexylpiperazin-1-yl)[1-(2-phenylethyl)-1H-1,2,3,4-tetrazol-5-yl]methyl]-6-methoxy-1,2-dihydroquinolin-2-one
Smiles: COC1=CC2C=C(C(C3=NN=NN3CCC3C=CC=CC=3)N3CCN(CC3)C3CCCCC3)C(=O)NC=2C=C1
InChiKey: ZVWPOIUAPXDLMB-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (94.76 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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%.
References:
- Kortagere S, et al. Identification of Novel Allosteric Modulators of Glutamate Transporter EAAT2. ACS Chem Neurosci. 2018 Mar 21;9(3):522-534.
Products are for research use only. Not for human use.
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