Bitopertin (R enantiomer)

• UNSPSC Description:

  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.

• Target Antigen:

  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 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]

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  9007-83-4