A selective inhibitor of GlyT1 (IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake; examined in clinical trials on persistent negative symptoms associated with schizophrenia

Bitopertin – 10 mg

Brand:
Cayman
CAS:
845614-11-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bitopertin is an inhibitor of the glycine transporter 1 (GlyT1; IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake.{33096} It is selective for GlyT1, inhibiting GlyT2 and off-target ERG channels with IC50 values of >30 and 17 µM, respectively.{33096} Bitopertin was examined in clinical trials on persistent negative symptoms associated with schizophrenia but failed to meet the primary endpoints set forth in these studies.{33097}  

 

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Description

A selective inhibitor of GlyT1 (IC50 = 30 nM) that increases levels of glycine by inhibiting its reuptake; examined in clinical trials on persistent negative symptoms associated with schizophrenia

Formal name: [4-[3-fluoro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl][5-(methylsulfonyl)-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]phenyl]-methanone

Synonyms:  RG-1678|RO-4917838

Molecular weight: 543.5

CAS: 845614-11-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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