Bitopertin (R enantiomer)

Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.

Product Specifications

CAS Number

[845614-12-2]

Product Name Alternative

RG1678 (R enantiomer) ; RO4917838 (R enantiomer)

UNSPSC

12352005

Target

GlyT

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Bitopertin-R-enantiomer.html

Purity

95.68

Solubility

10 mM in DMSO

Smiles

FC1=CC(C(F)(F)F)=CN=C1N2CCN(C(C3=CC(S(=O)(C)=O)=CC=C3O[C@@H](C(F)(F)F)C)=O)CC2

Molecular Formula

C21H20F7N3O4S

Molecular Weight

543.46

References & Citations

[1]Alberati D, et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment of schizophrenia. Neuropharmacology. 2012 Feb;62 (2) :1152-61.|[2]Pinard E, et al. Selective GlyT1 Inhibitors: Discovery of [4- (3-Fluoro-5-trifluoromethylpyridin-2-yl) piperazin-1-yl][5-methanesulfonyl-2- ((S) -2,2,2-trifluoro-1-methylethoxy) phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia. J Me|[3]Alberati, Daniela; Moreau, Jean-Luc; Lengyel, Judith et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment of schizophrenia. Neuropharmacology (2012), 62 (2), 1152-1161.|[4]Hofmann C, Banken L, Hahn M et al. Evaluation of the Effects of Bitopertin (RG1678) on Cardiac Repolarization: A Thorough Corrected QT Study in Healthy Male Volunteers. Clin Ther. 2012 Oct;34 (10) :2061-71.|[5]Martin-Facklam M, Pizzagalli F, Zhou Y et al. Glycine Transporter Type 1 Occupancy by Bitopertin: a Positron Emission Tomography Study in Healthy Volunteers. Neuropsychopharmacology. 2012 Nov 7. doi: 10.1038/npp.2012.212. [Epub ahead of print]