Home Neuronal Signaling GlyT inhibitor - Amino acid transporter inhibitor Bitopertin For research use only.

Bitopertin

Synonyms: RG1678, RO-4917838

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

Bitopertin Chemical Structure

CAS No. 845614-11-1

Purity & Quality Control

Batch: S821901 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.80%
99.80

Bitopertin Related Products

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
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
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].
Animal Research Animal Models Mice
Dosages 0.3-30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05883748 Enrolling by invitation
Erythropoietic Protoporphyria
Disc Medicine Inc
 August 31 2023 Phase 2|Phase 3
NCT05828108 Recruiting
Steroid-refractory Diamond-Blackfan Anemia (DBA)
National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)
 July 25 2023 Phase 1|Phase 2
NCT05308472 Active not recruiting
Erythropoietic Protoporphyria
Disc Medicine Inc
 October 31 2022 Phase 2
NCT03271541 Completed
Beta-Thalassemia
Hoffmann-La Roche
 October 26 2017 Phase 2
NCT02019290 Withdrawn
Healthy Volunteer
Hoffmann-La Roche
 February 10 2014 Phase 1
NCT01674361 Completed
Obsessive-Compulsive Disorder
Hoffmann-La Roche
 December 31 2012 Phase 2

Chemical Information & Solubility

Molecular Weight 543.46 Formula

C21H20F7N3O4S
CAS No. 845614-11-1 SDF Download Bitopertin SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (184.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Bitopertin | Bitopertin supplier | purchase Bitopertin | Bitopertin cost | Bitopertin manufacturer | order Bitopertin | Bitopertin distributor