ASP-2535

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H18N6O
Molecular Weight	382.4179
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(C)C1=NN=C(N1C2=CC=CC3=NON=C23)C4=CC=C(N=C4)C5=CC=CC=C5

InChI

InChIKey=FQGLDGKVKDPVLO-UHFFFAOYSA-N

InChI=1S/C22H18N6O/c1-14(2)21-24-25-22(28(21)19-10-6-9-18-20(19)27-29-26-18)16-11-12-17(23-13-16)15-7-4-3-5-8-15/h3-14H,1-2H3

HIDE SMILES / InChI

Description

ASP-2535 is a glycine transporter-1 (GlyT1) inhibitor which was developed by Astellas Pharma for the treatment of Schizophrenia and Alzheimer's disease. Although ASP-2535 was shown to improve cognitive impairment in animal models, it is no longer in the company pipeline.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glycine transporter 1 9	Inhibitor 8,504		92.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alzheimer’s disease 278	Primary		Preclinical	Unknown
Schizophrenia 305	Primary		Preclinical	Unknown

PubMed

Show entries

Title	Date	PubMed
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 disease.	2012 Jun 15	22542656

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Patents

Sample Use Guides

In Vivo Use Guide

Rats were given ASP-2535 at a dose of 0.1-3 mg/kg

Route of Administration: Oral

In Vitro Use Guide

Unknown

Show entries

Name

Type

Language

2,1,3-BENZOXADIAZOLE, 4-(3-(1-METHYLETHYL)-5-(6-PHENYL-3-PYRIDINYL)-4H-1,2,4-TRIAZOL-4-YL)-

Preferred Name

English

ASP-2535

Common Name

English

4-(3-(1-METHYLETHYL)-5-(6-PHENYL-3-PYRIDINYL)-4H-1,2,4-TRIAZOL-4-YL)-2,1,3-BENZOXADIAZOLE

Systematic Name

English

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Code System

Code

Type

Description

PUBCHEM

9800113

PRIMARY

FDA UNII

6627LI8F9K

PRIMARY

CAS

374886-51-8

PRIMARY

MANUFACTURER PRODUCT INFORMATION

ASP-2535

PRIMARY

ASP 2535: Cat. No. 5308Biological 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.

SMS_ID

300000042369

PRIMARY

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ACTIVE MOIETY


					6627LI8F9K

ASP-2535

SMILES

InChI

Description<div class="info-popup-container"><div><span class="pop-sub-key ">Sources:&nbsp;</span><span class="pop-sub-val"><span class="ext-link"><a target="_self" href="https://www.ncbi.nlm.nih.gov/pubmed/22542656">https://www.ncbi.nlm.nih.gov/pubmed/22542656</a></span></span></div></div>

CNS Activity

Originator

Approval Year

Targets

Conditions

PubMed

Patents

Sample Use Guides

Description