| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Ro 15-3890 targets the benzodiazepine site on the GABAA receptor. As a benzodiazepine receptor antagonist, it binds to the same site as benzodiazepines but does not activate the receptor. It acts as a blocker (antagonist) at the GABAA receptor. It is the primary metabolite of flumazenil and has similar receptor-binding properties, though with lower potency.
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| ln Vitro |
In vitro, Ro 15-3890 binds to the benzodiazepine receptor. Its binding affinity is lower than that of the parent compound flumazenil. It acts as a GABAA receptor blocker. Its activity is confirmed in radioligand binding assays using membrane preparations from brain tissue expressing GABAA receptors. Its purity is >98%.
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| ln Vivo |
In vivo, Ro 15-3890 is the primary metabolite of flumazenil. As a metabolite, it contributes to the pharmacological profile of flumazenil. It is not used as a therapeutic agent on its own. Its presence in the body reflects the metabolism of flumazenil.
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| Enzyme Assay |
Cell-free assays for Ro 15-3890 are radioligand binding assays using membrane preparations from brain tissue or cells expressing GABAA receptors. The compound's binding affinity is determined by its ability to displace a labeled benzodiazepine receptor ligand such as [3H]flumazenil. Its molecular weight (275.24) and formula (C13H10FN3O3) are confirmed by mass spectrometry.
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| Cell Assay |
Cellular assays for Ro 15-3890 are performed using cells expressing GABAA receptors. Cells are treated with varying concentrations of Ro 15-3890, and its ability to antagonize benzodiazepine-induced potentiation of GABA responses is assessed using electrophysiological techniques or calcium imaging. Its antagonist activity is confirmed.
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| Animal Protocol |
In vivo animal experiments for Ro 15-3890 are not typically conducted because it is a metabolite. Studies of flumazenil metabolism measure the levels of Ro 15-3890 in plasma and tissues following flumazenil administration. Its pharmacokinetic properties are derived from these studies.
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| ADME/Pharmacokinetics |
Ro 15-3890 has a molecular weight of 275.24 g/mol and a molecular formula of C13H10FN3O3. It is a solid powder. It has a purity of >98%. It is soluble in DMSO and should be stored under recommended conditions. Its chemical name is 8-fluoro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid.
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| Toxicity/Toxicokinetics |
The toxicological profile of Ro 15-3890 is consistent with that of flumazenil and its metabolites. It is generally well-tolerated. No significant toxicity has been reported. Its safety is established through the clinical use of flumazenil.
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| References |
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| Additional Infomation |
Ro 15-3890 is the primary carboxylic acid metabolite of flumazenil (Ro 15-1788), a benzodiazepine antagonist. It is also known as flumazenil acid and desethylflumazenyl. It acts as a benzodiazepine receptor antagonist. It is a research compound and is not used as a therapeutic agent.
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| Molecular Formula |
C13H10FN3O3
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|---|---|
| Molecular Weight |
275.24
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| Exact Mass |
275.07
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| CAS # |
84378-44-9
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| PubChem CID |
134757
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
570.5±50.0 °C at 760 mmHg
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| Flash Point |
298.8±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
-0.16
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
433
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
Ro-15-3890; Ro 153890; Ro 15-3890
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~363.32 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6332 mL | 18.1660 mL | 36.3319 mL | |
| 5 mM | 0.7266 mL | 3.6332 mL | 7.2664 mL | |
| 10 mM | 0.3633 mL | 1.8166 mL | 3.6332 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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