374886-51-8

374886-51-8 structure

Name: ASP 2535
Chemical Name: 4-[3-Isopropyl-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole
CAS Number: 374886-51-8
Molecular Formula: C₂₂H₁₈N₆O
Molecular Weight: 382.418
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GlyT
Create Date: 2020-01-11 21:04:57
Modify Date: 2024-04-05 17:00:59
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

Name	4-[3-Isopropyl-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole
Synonyms	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

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