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 Peso molecular: 303.29 Número EC: 616-650-9
Disponible para pedir
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
Estado
Price
Qty
1ml
F408716-1ml
2

92,90US$

134,90US$
Guardar 42,00 US$ (31.13%)
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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.

Descripción general

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

Sinónimos
4H-Imidazo[1, 5-a][1, 4]benzodiazepine-3-carboxylic acid, 8-fluoro-5, 6-dihydro-5-methyl-6-oxo-, ethyl ester
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Grado
Moligand™
Tipo de acción
ALLOSTERIC MODULATOR
Mecanismo de acción
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;
Propiedades del producto
ALogP1
Nombres e identificadores
Isómeros SMILES CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)F)C
WGK Alemania 2
RTECS NI2922170
CAS alternativo 78755-81-4
Número NSC 759193
Términos de entrada MeSH Anexate;Flumazenil;Flumazepil;Lanexat;Ro 15 1788;Ro 15-1788;Ro 151788;Romazicon
Peso molecular 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

Objetivos asociados (humanos)
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)
Certificados (CoA, COO, BSE/TSE y tabla de análisis)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propiedades químicas y físicas
SolubilidadSolubility (25°C) In vitro DMSO: 57 mg/mL (199.1 mM);    
Índice de refracción1.63
Punto de ebullición (°C)527.98 °C at 760 mmHg
Punto de fusión (°C)200 °C
Citations of This Product
Referencias
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]
Calculadoras de soluciones
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