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Description: Potent and selective GlyT1 inhibitor
Chemical Name: 4-[3-(1-Methylethyl)-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole
Purity: ≥98% (HPLC)
Biological Activity for ASP 2535
ASP 2535 is a potent and selective GlyT1 inhibitor (IC50 = 92 nM). Exhibits 50-fold selectivity over GlyT2. Attenuates MK 801-induced working memory deficits and PCP-induced visual learning deficits in mice. Orally available and brain penetrant.
Compound Libraries for ASP 2535
ASP 2535 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for ASP 2535
| M. Wt | 382.42 |
| Formula | C22H18N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 374886-51-8 |
| PubChem ID | 9800113 |
| InChI Key | FQGLDGKVKDPVLO-UHFFFAOYSA-N |
| Smiles | CC(C)C1=NN=C(C4=CN=C(C5=CC=CC=C5)C=C4)N1C3=CC=CC2=NON=C23 |
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 ASP 2535
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.24 | 100 | |
| ethanol | 38.24 | 100 |
Preparing Stock Solutions for ASP 2535
The following data is based on the product molecular weight 382.42. 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 | 2.61 mL | 13.07 mL | 26.15 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.23 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets for ASP 2535
References for ASP 2535
References are publications that support the biological activity of the product.
Harada et al (2012) A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's diseas Eur.J.Pharmacol. 685 59 PMID: 22542656
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Keywords: ASP 2535, ASP 2535 supplier, ASP2535, potent, selective, glycine, transporters, GlyT1, inhibitors, inhibits, schizophrenia, alzheimer's, disease, Glycine, Transporters, 5308, Tocris Bioscience
1 Citation for ASP 2535
Citations are publications that use Tocris products. Selected citations for ASP 2535 include:
Rita U et al (2014) Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation. J Biomed Sci 21 74 PMID: 25096780
Do you know of a great paper that uses ASP 2535 from Tocris? Please let us know.
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