| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Radequinil targets the benzodiazepine receptor (BzR), which is a modulatory site on the GABAA receptor complex. The GABAA receptor is a ligand-gated ion channel that mediates inhibitory neurotransmission in the central nervous system. Benzodiazepines bind to the BzR and enhance the effects of GABA, leading to increased chloride influx and neuronal inhibition. Radequinil is a partial inverse agonist at the BzR, meaning it binds to the receptor and produces effects that are opposite to those of full agonists like diazepam, but with less efficacy than a full inverse agonist. It binds to GABA(-) and GABA(+) ligands with Ki values of 5.15 and 6.11 nM, respectively. By acting as a partial inverse agonist, Radequinil modulates GABAA receptor function and may enhance cognitive function or modulate anxiety.
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| ln Vitro |
In vitro studies have characterized Radequinil as a benzodiazepine receptor partial inverse agonist. Its activity is typically measured using receptor binding assays and functional assays. In receptor binding assays, Radequinil competes with radiolabeled ligands for binding to the BzR, with Ki values of 5.15 and 6.11 nM for GABA(-) and GABA(+) ligands, respectively. In functional assays, the compound's effects on GABAA receptor-mediated chloride flux are measured. As a partial inverse agonist, Radequinil reduces the chloride influx induced by GABA, but to a lesser extent than a full inverse agonist. These in vitro studies confirm that Radequinil is a potent and selective modulator of the BzR.
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| ln Vivo |
In vivo studies have demonstrated that Radequinil modulates anxiety- and cognition-related behaviors. It is used to probe GABAA receptor-mediated neurotransmission and anxiety- or cognition-related circuitry. The compound has been investigated for the potential treatment of Alzheimer's disease, suggesting that it may have cognitive-enhancing effects. However, specific in vivo protocols and results are not extensively detailed in the available literature. Radequinil is a research tool for studying the role of benzodiazepine receptors in cognition and anxiety.
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| Enzyme Assay |
The in vitro receptor binding assays for Radequinil measure its affinity for the benzodiazepine receptor (BzR). In a typical assay, membranes are prepared from brain tissue (e.g., rat cerebral cortex) and incubated with a radiolabeled ligand that binds to the BzR, such as [3H]flumazenil or [3H]diazepam. Increasing concentrations of unlabeled Radequinil are added to compete with the radiolabeled ligand for binding. After incubation, the bound and free ligand are separated by filtration, and the radioactivity is measured. The Ki values are determined from the competition curves. For Radequinil, the Ki values for GABA(-) and GABA(+) ligands are 5.15 and 6.11 nM, respectively. These assays provide a quantitative measure of Radequinil's affinity for the BzR.
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| Cell Assay |
In vitro cell-based assays for Radequinil are used to study its functional effects on GABAA receptors. A common assay is the measurement of chloride flux in cells expressing GABAA receptors. Cells are loaded with a chloride-sensitive fluorescent dye, and the change in fluorescence is measured upon GABA stimulation in the presence or absence of Radequinil. As a partial inverse agonist, Radequinil reduces the GABA-induced chloride influx. Alternatively, electrophysiological techniques, such as patch-clamp, can be used to directly measure the chloride current through GABAA receptors. These cell-based assays confirm that Radequinil modulates GABAA receptor function.
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| Animal Protocol |
In vivo animal experiments for Radequinil are conducted to study its effects on behavior and cognition. In a typical study, Radequinil is administered to rats or mice, and its effects are assessed in behavioral tests. For anxiety, tests such as the elevated plus maze or the light-dark box are used. For cognition, tests such as the Morris water maze or the novel object recognition test are used. Radequinil is used to probe GABAA receptor-mediated neurotransmission and anxiety- or cognition-related circuitry. The compound has been investigated for the potential treatment of Alzheimer's disease, suggesting that it may have cognitive-enhancing effects in animal models.
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| ADME/Pharmacokinetics |
Radequinil has a molecular weight and formula that are not specified in the available literature, but based on its structure, it has a molecular formula of C18H16N4O3. For research use, Radequinil is typically supplied as a powder. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the compound at -20°C in a dry, dark environment. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied. Radequinil is a small, lipophilic molecule that is expected to cross the blood-brain barrier.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Radequinil is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vivo studies have used Radequinil at doses that modulate behavior without apparent toxicity. However, comprehensive toxicological studies, including acute and chronic toxicity studies, have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling Radequinil. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
Radequinil (AC-3933) is a research compound and is not approved for any clinical or therapeutic use. It is a benzodiazepine receptor (BzR) partial inverse agonist. Radequinil binds to GABA(-) and GABA(+) ligands with Ki values of 5.15 and 6.11 nM, respectively. It is used to probe GABAA receptor-mediated neurotransmission and anxiety- or cognition-related circuitry. The compound has been investigated for the potential treatment of Alzheimer's disease. Radequinil's mechanism of action involves modulating GABAA receptor function by acting as a partial inverse agonist at the benzodiazepine binding site. This modulation can affect anxiety, cognition, and other behaviors.
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| Molecular Formula |
C18H14N4O3
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| Molecular Weight |
334.335
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| Exact Mass |
334.106
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| CAS # |
219846-31-8
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| PubChem CID |
135418404
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.620
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| LogP |
2.54
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
540
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JQOFKKWHXGQABB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14N4O3/c1-10-20-17(22-25-10)14-9-13-15(21-18(14)23)6-7-19-16(13)11-4-3-5-12(8-11)24-2/h3-9H,1-2H3,(H,21,23)
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| Chemical Name |
5-(3-methoxyphenyl)-3-(5-methyl-1,2,4-oxadiazol-3-yl)-1H-1,6-naphthyridin-2-one
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| Synonyms |
AC3933 AVE3933AC 3933 AVE 3933Radequinil AC-3933 AVE-3933 SX-3933 SX3933 SX 3933
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~10 mg/mL (~29.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9910 mL | 14.9548 mL | 29.9097 mL | |
| 5 mM | 0.5982 mL | 2.9910 mL | 5.9819 mL | |
| 10 mM | 0.2991 mL | 1.4955 mL | 2.9910 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00359944 | COMPLETEDWITH RESULTS | Drug: AC-3933 Drug: AC-3933 Other: Sugar Pill |
Alzheimer's Disease | Sumitomo Pharma America, Inc. | 2006-02 | Phase 2 |
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