ASP 2535

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Cat.No. 5308 - ASP 2535 | C22H18N6O | CAS No. 374886-51-8
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.24 100
ethanol 38.24 100

Preparing Stock Solutions

The following data is based on the product molecular weight 382.42. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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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Citations for ASP 2535

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Literature in this Area

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Schizophrenia

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.