Flumazenil (RO 15-1788) - Moligand™, 10mM in DMSO , Allosteric modulator of GABA A receptor α1 subunit;Allosteric modulator of GABA A receptor α2 subunit;Allosteric modulator of GABA A receptor α3 subunit;Allosteric modulator of GABA A receptor α4 subunit, Allosteric modulator of GABA A receptor α1 subunit;Allosteric modulator of GABA A receptor α2 subunit;Allosteric modulator of GABA A receptor α3 subunit;Allosteric modulator of GABA A receptor α4 subunit;Allosteric modulator of GABA A receptor α5 subunit;

CAS: 78755-81-4 Cat. No.: F408716 Molecular Weight: 303.29 EC Number: 616-650-9
AVAILABLE TO ORDER
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
4H-Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
 ·  off list, applied to all prices below.
Size
Status
Price
Qty
1ml
F408716-1ml
2

$92.90

$134.90
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 4 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

Information

Flumazenil (RO 15-1788) is a competitiveGABAA receptorantagonist, used in the treatment of benzodiazepine overdoses.
In vitro


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. Flumazenil 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. Flumazenil 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. Flumazenil (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test. Flumazenil (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats. Flumazenil (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. Flumazenil slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test. Flumazenil (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.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

Specifications

Synonyms
4H-Imidazo[1, 5-a][1, 4]benzodiazepine-3-carboxylic acid, 8-fluoro-5, 6-dihydro-5-methyl-6-oxo-, ethyl ester
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR
Mechanism of action
Allosteric modulator of GABA A receptor α1 subunit;Allosteric modulator of GABA A receptor α2 subunit;Allosteric modulator of GABA A receptor α3 subunit;Allosteric modulator of GABA A receptor α4 subunit;Allosteric modulator of GABA A receptor α5 subunit;
Product Properties
ALogP1
Names and Identifiers
Isomeric SMILES CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)F)C
WGK Germany 2
RTECS NI2922170
Alternate CAS 78755-81-4
NSC Number 759193
MeSH Entry Terms Anexate;Flumazenil;Flumazepil;Lanexat;Ro 15 1788;Ro 15-1788;Ro 151788;Romazicon
Molecular Weight 303.29
Reaxy-Rn 4763661
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4763661&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Associated Targets(Human)
GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GABRA3 Tclin Gamma-aminobutyric acid receptor subunit alpha-3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GABRA4 Tclin Gamma-aminobutyric acid receptor subunit alpha-4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GABRA5 Tclin Gamma-aminobutyric acid receptor subunit alpha-5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GABRA2 Tclin Gamma-aminobutyric acid receptor subunit alpha-2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GABRA6 Tclin Gamma-aminobutyric acid receptor subunit alpha-6 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificates(CoA,COO,BSE/TSE and Analysis Chart)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemical and Physical Properties
SolubilitySolubility (25°C) In vitro DMSO: 57 mg/mL (199.1 mM);    
Refractive Index1.63
Boil Point(°C)527.98 °C at 760 mmHg
Melt Point(°C)200 °C
Citations of This Product
References
1. Niping Li, Yaorong Yang, Shengyuan Zhang, Bin Jiang, Wei Zhang, Haibo Wang, Lixin Chen, Liwei Wang, Yiyi Li, Lei Shi, Wencai Ye, Lei Wang.  (2025)  The toxic components, toxicological mechanism and effective antidote for Gelsemium elegans poisoning.  Acta Pharmaceutica Sinica B,      [PMID:41049747] [10.1016/j.apsb.2025.07.016]
2. Jing Jiang, Zhao-liang Hu, Hamza Boucetta, Jia-ming Liu, Min Song, Tai-jun Hang, Yu-ting Lu.  (2022)  Identification of degradation products in flumazenil using LC-Q-TOF/MS and NMR: Degradation pathway elucidation.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:35447492] [10.1016/j.jpba.2022.114764]
3. Nan Zhang, Mu Luo, Lei He, Lei Yao.  (2020)  Chemical Composition of Essential Oil from Flower of ‘Shanzhizi’ (Gardenia jasminoides Ellis) and Involvement of Serotonergic System in Its Anxiolytic Effect.  MOLECULES,  25  (20): (4702).  [PMID:33066512] [10.3390/molecules25204702]
4. Kai Zhang, Jing Lu, Lei Yao.  (2019)  Involvement of the dopamine D1 receptor system in the anxiolytic effect of cedrol in the elevated plus maze and light–dark box tests.  JOURNAL OF PHARMACOLOGICAL SCIENCES,      [PMID:31786058] [10.1016/j.jphs.2019.11.004]
Solution Calculators
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