Bitopertin R enantiomer Inhibitor

Name: Bitopertin R enantiomer Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5752801
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752801

Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a noncompetitive glycine reuptake inhibitor and inhibits glycine uptake at human GlyT1 (IC50: 25nM). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

Bitopertin R enantiomer, Inhibitor

Full Product Name

Bitopertin R enantiomer

Product Synonym Names

RG1678 (R enantiomer); RO4917838 (R enantiomer)

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

543.46

Solubility

<1mg/ml refers to the product slightly soluble or insoluble

Formula

C21H20F7N3O4S

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

CAS Number

845614-12-2

Target & IC50

GlyT1: ic50 25nM

In Vitro

Bitopertin dose-dependently increases cerebrospinal fluid and striatal levels of glycine measured by microdialysis in rats. Additionally, Bitopertin attenuates hyperlocomotion induced by the psychostimulant D-amphetamine or thenMDA receptor glycine site antagonist L-687,414 in mice. Bitopertin also prevents the hyper-response to the D-amphetamine challenge in rats treated chronically with phencyclidine. The administration of vehicle has no effect on extracellular levels of striatal glycine, which remained constant throughout the experiment. In contrast, p.o. administration of Bitopertin (1-30mg/kg) produced a dose-dependent increase in extracellular glycine levels. Bitopertin (30mg/kg) produces glycine levels 2.5 times higher than pretreatment,levels. A similar dose-dependent increase in glycine concentration is observed in the CSF of rats treated p.o. with Bitopertin (1-10mg/kg) compared with vehicle-treated animals, 3 hours after drug administration [1]. In vivo pharmacokinetic studies in rat and monkey reveals that Bitopertin has, in both species, a low plasma clearance, an intermediate volume of distribution, a good oral bioavailability (78% for rat, 56% for monkey), and a favorable terminal half-life (5.8 h for rat, 6.4 h for monkey). The plasma protein binding is high in the two preclinical species (97%) and in human (98%). The CNS penetration of Bitopertin in rat (brain/plasma=0.7) is better than that in mouse (brain/plasma=0.5) [2].

Product Categories/Family for Bitopertin R enantiomer, inhibitor

Neuroscience; GlyT

Product References and Citations for Bitopertin R enantiomer, inhibitor

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.
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.
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
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
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.
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.
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.
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.
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]
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]

Other Notes

Small volumes of Bitopertin R enantiomer, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Bitopertin R enantiomer purchase

MBS5752801 is an inhibitor targeting Bitopertin R enantiomer.