research use only

Flumazenil GABA Receptor antagonist

Cat.No.S1332

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Jump to

Quality Control

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (329.71 mM) Warmed with 60°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

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.

Chemical Information, Storage & Stability

Molecular Weight 303.29 Formula

C15H14FN3O3

Storage (From the date of receipt)
CAS No. 78755-81-4 Download SDF Storage of Stock Solutions

Synonyms RO 15-1788 SMILES CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)F)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
GABAA receptor
In vivo
Flumazenil interacts at the central benzodiazepine receptor to antagonize or reverse the behavioral, neurologic, and electrophysiologic effects of benzodiazepine agonists and inverse agonists. This compound is of some benefit in hepatic encephalopathy, but until well-designed clinical trials are conducted, hepatic encephalopathy must be considered an investigational indication for flumazenil. It has been shown to reverse sedation caused by intoxication with benzodiazepines alone or benzodiazepines in combination with other agents, but it should not be used when cyclic antidepressant intoxication is suspected. This chemical (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test. It (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats. This compound (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. It slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test. This chemical (3.0 mg/kg) blocks the changes withdrawal from chronic ethanol treatment, which leads to a decrease in open arm time and percent open arm entries.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7889291/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9226737/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-01)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07619092 RECRUITING
Depression - Major Depressive Disorder; Bipolar Disorder (BD); Functional Magnetic Resonance Imaging (fMRI); Cognition; Autobiographical Memory; Electroconvulsive Therapy; ECT; Treatment Outcome; Inpatients
Anders Jørgensen
2026-01-15
NCT07663877 NOT_YET_RECRUITING
Hysteroscopy; Ambulatory Surgery; General Anesthesia
Chung-Ang University Gwangmyeong Hospital
2026-06 PHASE4
NCT07265050 NOT_YET_RECRUITING
Emergence Agitation
Seoul National University Hospital
2026-01-01
NCT07277881 NOT_YET_RECRUITING
Postoperative Delirium; Sedation; Remimazolam; Hip Arthroplasty, Total
Medical University of Gdansk
2026-01 PHASE4
NCT05939674 RECRUITING
Flumazenil Adverse Reaction; Remimazolam; Hip Joint; Elderly Patients
Pusan National University Yangsan Hospital
2023-09-19
NCT06531369 UNKNOWN
Flumazenil to Antagonize Remimazolam; Remimazolam; Renal Transplantation
Qianfoshan Hospital
2024-07 PHASE1

Read more about Clinical Trials

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map