Bitopertin

Catalog No.S8219 Synonyms: RG1678, RO-4917838

For research use only.

Bitopertin (RG1678,RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.

Bitopertin Chemical Structure

CAS No. 845614-11-1

Selleck's Bitopertin has been cited by 1 Publication

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Choose Selective GlyT Inhibitors

Biological Activity

Description Bitopertin (RG1678,RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.
Targets
GlyT1 [1]
(in cells stably expressing mGlyT1b)
GlyT1 [1]
(in cells stably expressing hGlyT1b)
22 nM 25nM
In vitro

RG1678 noncompetitively inhibits [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 displaces [3H]ORG24598 binding with a Ki of 8.1 nM at human hGlyT1b in membranes from Chinese hamster ovary cells. RG1678 has no effect on hGlyT2-mediated [3H]glycine uptake up to 30 μM concentration. There is no significant species difference in the pharmacology for RG1678 based on the ability of the compound to displace [3H]ORG24598. In hippocampal CA1 pyramidal cells, RG1678 enhances NMDA-dependent long-term potentiation (LTP) at 30 nM (213 ± 18%; n=7), 100 nM (269 ± 44%, n=13) but not at 300 nM (152 ± 14%; n = 9)[1].

In vivo Administration of RG1678 produces a long-lasting (>3h) dose-dependent increase in extracellular glycine levels both in microdialysis experiments conducted in rats and CSF of rats. In mice, RG1678 dose-dependently and significantly attenuates hyperlocomotion induced by the psychostimulant D-amphetamine. RG1678 also prevents the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker[1].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Mice
  • Dosages: 0.3-30 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 543.46
Formula

C21H20F7N3O4S

CAS No. 845614-11-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(F)(F)F)OC1=C(C=C(C=C1)S(=O)(=O)C)C(=O)N2CCN(CC2)C3=C(C=C(C=N3)C(F)(F)F)F

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03271541 Completed Drug: Bitopertin Beta-Thalassemia Hoffmann-La Roche October 26 2017 Phase 2
NCT02019290 Withdrawn Drug: Midazolam|Drug: bitopertin Healthy Volunteer Hoffmann-La Roche February 10 2014 Phase 1
NCT01674361 Completed Drug: Bitopertin|Drug: Placebo|Drug: SSRI Obsessive-Compulsive Disorder Hoffmann-La Roche December 31 2012 Phase 2
NCT01665976 Completed Drug: RO4917838|Drug: RO4927838 Healthy Volunteer Hoffmann-La Roche August 2012 Phase 1
NCT01543529 Completed Drug: RO4917838|Drug: Placebo to RO4917838|Other: Alcohol Healthy Volunteer Hoffmann-La Roche February 28 2012 Phase 1
NCT01510899 Completed Drug: RO4917838 Healthy Volunteer Hoffmann-La Roche October 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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