Bitopertin

Catalog No.S8219 Synonyms: RG1678, RO-4917838

Bitopertin Chemical Structure

Molecular Weight(MW): 543.46

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.

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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

Animal Research:

[1]

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  • Animal Models: Mice
  • Formulation: H2O with 0.3% Tween 80
  • Dosages: 0.3-30 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (184.0 mM)
Ethanol 100 mg/mL (184.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 543.46
Formula

C21H20F7N3O4S

CAS No. 845614-11-1
Storage powder
in solvent
Synonyms RG1678, RO-4917838

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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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID