SML2823
GT949
≥98% (HPLC)
Synonym(s):
3-[(4-Cyclohexyl-1-piperazinyl)[1-(2-phenylethyl)-1H-tetrazol-5-yl]methyl]-6-methoxy-2(1H)-quinolinone, GT 949, GT-949
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About This Item
Empirical Formula (Hill Notation):
C30H37N7O2
CAS Number:
Molecular Weight:
527.66
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C1C(C(C2=NN=NN2CCC3=CC=CC=C3)N4CCN(CC4)C5CCCCC5)=CC6=CC(OC)=CC=C6N1
Biochem/physiol Actions
GT949 is a potent and selective positive allosteric modulator (PAM) of the excitatory amino acid transporter EAAT2 (glutamate uptake EC50 = 0.26 nM; COS-7 EAAT2 transfectant), but not EAAT1 or EAAT3. GT949 enhances glutamate uptake of cultured rat astrocytes (EC50 = 1 nM, Emax = 158%) with no potency toward human serotonin (SERT), noradrenaline (NET) and dopamine (DAT) transporters, nor NMDA receptors (murine primary cortical neurons).
Potent and selective positive allosteric modulator (PAM) of the excitatory amino acid transporter EAAT2, but not EAAT1, EAAT3, NMDAR, SERT, NET, or DAT.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Sandhya Kortagere et al.
ACS chemical neuroscience, 9(3), 522-534 (2017-11-16)
Dysfunction of excitatory amino acid transporters (EAATs) has been implicated in the pathogenesis of various neurological disorders, such as stroke, brain trauma, epilepsy, and neurodegenerative diseases, among others. EAAT2 is the main subtype responsible for glutamate clearance in the brain
Romulo Martelli Falcucci et al.
ACS chemical neuroscience, 10(8), 3437-3453 (2019-07-02)
Dysfunction of excitatory amino acid transporters (EAATs) has been implicated in the pathogenesis of various neurological disorders, such as stroke, brain trauma, epilepsy, and several neurodegenerative disorders. EAAT2 is the main transporter subtype responsible for glutamate clearance in the brain
Rong-Wei Zhang et al.
Cell reports, 27(10), 2871-2880 (2019-06-06)
Retinal waves, the spontaneous patterned neural activities propagating among developing retinal ganglion cells (RGCs), instruct the activity-dependent refinement of visuotopic maps. Although it is known that the wave is initiated successively by amacrine cells and bipolar cells, the behavior and
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML2823-25MG | 04061842610846 |
| SML2823-5MG | 04061842610853 |
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