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SML2823

Sigma-Aldrich

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:
460330-27-2
Molecular Weight:
527.66
MDL number:
MFCD03129031
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

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).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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

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