A positive allosteric modulator of EEAT2
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GT 949

Item No. 34552

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(4-cyclohexyl-1-piperazinyl)[1-(2-phenylethyl)-1H-tetrazol-5-yl]methyl]-6-methoxy-2(1H)-quinolinone
CAS Number
460330-27-2
Molecular Formula
C30H37N7O2
Formula Weight
527.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 10 mM, heated
SMILES
O=C1NC2=C(C=C1C(C3=NN=NN3CCC4=CC=CC=C4)N5CCN(C6CCCCC6)CC5)C=C(OC)C=C2
InChi Code
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)
InChi Key
ZVWPOIUAPXDLMB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    Product Description

    GT 949 is a positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2; EC50 = 0.26 nM for stimulating glutamate uptake by COS-7 cells expressing EAAT2).1 It is selective for EEAT2 over the serotonin (5-HT) transporter (SERT), the norepinephrine transporter (NET), and the dopamine transporter (DAT; IC50s = >1 mM for all). GT 949 (10 nM) reduces neuronal death induced by L-glutamate, but not hydrogen peroxide, in primary embryonic rat neuron-glia cultures.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kortagere, S., Mortensen, O.V., Xia, J., et al. Identification of novel allosteric modulators of glutamate transporter EAAT2. ACS Chem. Neurosci. 9(3), 522-534 (2018).

    2. Falcucci, R.M., Wertz, R., Green, J.L., et al. Novel positive allosteric modulators of glutamate transport have neuroprotective properties in an in vitro excitotoxic model. ACS Chem. Neurosci. 10(8), 3437-3453 (2019).