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Submit ReviewGT 949
Description: Potent and selective positive allosteric modulator of EAAT2
Chemical Name: 3-((4-Cyclohexylpiperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6-methoxyquinolin-2(1H)-one
Purity: ≥98% (HPLC)
Biological Activity for GT 949
GT 949 is a potent and selective EAAT2 positive allosteric modulator (EC50 = 0.26 nM). Enhances the glutamate translocation rate, with no effect on substrate interaction. Enhances glutamate uptake by cultured astrocytes by approximately 58%. Exhibits no significant effect on DAT, SERT and NET or NMDA receptors. Neuroprotective in an in vitro model of excitotoxicity.
Compound Libraries for GT 949
GT 949 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GT 949
| M. Wt | 527.66 |
| Formula | C30H37N7O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 460330-27-2 |
| PubChem ID | 3195790 |
| InChI Key | ZVWPOIUAPXDLMB-UHFFFAOYSA-N |
| Smiles | COC1=CC=C2NC(C(C(C3=NN=NN3CCC4=CC=CC=C4)N5CCN(C6CCCCC6)CC5)=CC2=C1)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GT 949
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 52.77 | 100 |
Preparing Stock Solutions for GT 949
The following data is based on the product molecular weight 527.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.9 mL | 9.48 mL | 18.95 mL |
| 5 mM | 0.38 mL | 1.9 mL | 3.79 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.9 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets for GT 949
References for GT 949
References are publications that support the biological activity of the product.
Kortagere et al (2018) Identification of novel allosteric modulators of glutamate transporter EAAT2. ACS Chem.Neurosci. 9 522 PMID: 29140675
Falcucci et al (2019) Novel Positive Allosteric Modulators of Glutamate Transport Have Neuroprotective Properties in an in Vitro Excitotoxic Model. ACS Chem.Neurosci. 10 3437 PMID: 31257852
If you know of a relevant reference for GT 949, please let us know.
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Keywords: GT 949, GT 949 supplier, GT949, selective, EAAT2, positive, allosteric, modulators, PAM, Glutamate, Transporters, 6578, Tocris Bioscience
1 Citation for GT 949
Citations are publications that use Tocris products. Selected citations for GT 949 include:
Zhang et al (2019) Müller Glial Cells Participate in Retinal Waves via Glutamate Transporters and AMPA Receptors. Cell Rep 27 2871 PMID: 31167134
Do you know of a great paper that uses GT 949 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Huntington's Disease Poster
Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.