ASP 2535 - 95%, high purity , CAS No.374886-51-8, Inhibitor of GlyT1

Item Number
A275113
Grouped product items
SKUSizeAvailabilityPrice Qty
A275113-1mg
1mg
Available within 8-12 weeks(?)
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$89.90
A275113-5mg
5mg
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$294.90
A275113-10mg
10mg
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$470.90

Potent and selective GlyT1 inhibitor

Basic Description

Synonyms4-[3-(1-Methylethyl)-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole
Specifications & PurityMoligand™, ≥95%
Biochemical and Physiological MechanismsIn vitro:ASP2535 potently inhibits rat GlyT1 (IC50=92 nM) with 50-fold selectivity over rat glycine transporter-2 (GlyT2) in vitro; In vivo:ASP2535 (1-3 mg/kg, p.o.) improves the PCP-induced deficit in prepulse inhibition in rats[1]. ASP2535 (0.3-3 mg/kg;
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of GlyT1
Product Description

ASP2535 is a potent, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor.ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.

Associated Targets(Human)

SLC6A9 Tchem Sodium- and chloride-dependent glycine transporter 1 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[3-(6-phenylpyridin-3-yl)-5-propan-2-yl-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole
INCHI 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
InChi Key FQGLDGKVKDPVLO-UHFFFAOYSA-N
Canonical SMILES CC(C)C1=NN=C(N1C2=CC=CC3=NON=C32)C4=CN=C(C=C4)C5=CC=CC=C5
Isomeric SMILES CC(C)C1=NN=C(N1C2=CC=CC3=NON=C32)C4=CN=C(C=C4)C5=CC=CC=C5
PubChem CID 9800113
Molecular Weight 382.42

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySoluble in DMSO to 75 mM and ethanol to 75 mM

Related Documents

References

1. Harada K, Nakato K, Yarimizu J, Yamazaki M, Morita M, Takahashi S, Aota M, Saita K, Doihara H, Sato Y 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 disease..  Eur J Pharmacol,  685  (1-3): (59-69).  [PMID:22542656] [10.1021/op500134e]

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