Bitopertin R enantiomer

• CAT Number: I005057
• CAS Number: 845614-12-2
• Molecular Formula: C21H20F7N3O4S
• Molecular Weight: 543.46
• Purity: ≥95%
• Target: GlyT1
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C

RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).IC50 value:Target: GlyT1In vitro, RG1678 noncompetitively inhibited [3H]glycine uptake in cells stably expressing hGlyT1b and mGlyT1b, with IC50 values of 25 ± 2 nM and 22 ± 5 nM, respectively (n = 6) and competitively displaced [3H]ORG24598 binding with a Ki of 8.1 nM at human hGlyT1b in membranes from Chinese hamster ovary cells.Recent Phase II data shows that RG1678 is effective in reducing the negative symptoms when given in combination with second generation antipsychotics. RG1678 is currently in Phase III trials for the treatment of the negative symptoms of schizophrenia.

Reference

[1]. Pinard, Emmanuel; Alanine, Alexander; Alberati, Daniela 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. Journal of Medicinal Chemistry (2010), 53(12), 4603-4614.
[2]. Hopkins, Corey R. ACS Chemical Neuroscience Molecule Spotlight on RG1678. ACS Chemical Neuroscience (2011), 2(12), 685-686.
[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]