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ASP 2535

Names

[ CAS No. ]:
374886-51-8

[ Name ]:
ASP 2535

[Synonym ]:
2,1,3-Benzoxadiazole, 4-[3-(1-methylethyl)-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-
4-[3-Isopropyl-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole

Biological Activity

[Description]:

A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2; shows minimal affinity for many other receptors except for μ-opioid receptors (IC50=1.83 uM); inhibits ex vivo [(3)H]-glycine uptake in mouse cortical homogenate, improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease. Schizophrenia Phase 1 Discontinued

[References]

References 1. Harada K, et al. Eur J Pharmacol. 2012 Jun 15;685(1-3):59-69. View Related Products by Target Glycine Transporter (GlyT) Schizophrenia

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
607.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H18N6O

[ Molecular Weight ]:
382.418

[ Flash Point ]:
321.1±34.3 °C

[ Exact Mass ]:
382.154205

[ LogP ]:
5.09

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.717

Related Compounds