ASP2535( ASP 2535 | ASP-2535 )

Catalog No. M14292 CAS No. 374886-51-8

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HNMR

HPLC

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Product Name

ASP2535
Note

Research use only, not for human use.
Brief 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.
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.
In Vitro

ASP2535 potently inhibits rat GlyT1 (IC50=92 nM) with 50-fold selectivity over rat glycine transporter-2 (GlyT2) in vitro.
In Vivo

ASP2535 (0.3-3 mg/kg; p.o) attenuates working memory deficit in MK-801-treated mice and visual learning deficit in neonatally phencyclidine (PCP)-treated mice.ASP2535 (1-3 mg/kg, p.o.) also improves the PCP-induced deficit in prepulse inhibition in rats. Animal Model:5-week-old male ddY mice Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg Administration:Oral administration Result:Significantly attenuated the MK-801-induced decrease in alternation rate.
Synonyms

ASP 2535 | ASP-2535
Pathway

Membrane Transporter/Ion Channel
Target

GlyT
Recptor

GlyT
Research Area

Neurological Disease
Indication

Schizophrenia

CAS Number

374886-51-8
Formula Weight

382.427
Molecular Formula

C22H18N6O
Purity

>98% (HPLC)
Solubility

——
SMILES

CC(C1=NN=C(C2=CC=C(C3=CC=CC=C3)N=C2)N1C4=CC=CC5=NON=C54)C
Chemical Name

4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole

1. Harada K, et al. Eur J Pharmacol. 2012 Jun 15;685(1-3):59-69.

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