| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
Clovoxamine targets the serotonin transporter (SERT) with a binding affinity Ki of 61 nM. It functions as a 5-hydroxytryptamine reuptake inhibitor and also inhibits norepinephrine reuptake. The compound has little affinity for muscarinic, histaminergic, serotonergic and adrenergic binding sites. As an SNRI, it increases synaptic levels of serotonin and norepinephrine, which is the basis for its antidepressant properties. The compound also exhibits anticonvulsant activity. Its mechanism involves inhibition of monoamine transporters without significant direct receptor interactions.
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| ln Vitro |
In vitro studies demonstrate that Clovoxamine has binding affinity for the serotonin transporter (SERT) with a Ki of 61 nM. It functions as a 5-HT and norepinephrine reuptake inhibitor. The compound exhibits antidepressant properties by enhancing serotonin and norepinephrine levels in the synaptic cleft. Clovoxamine induces a decrease in the functional beta-adrenergic receptor coupled c-AMP response. It has little affinity for muscarinic, histaminergic, serotonergic and adrenergic binding sites. The compound shows anticonvulsant activity in addition to its antidepressant effects.
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| ln Vivo |
In vivo studies of Clovoxamine were conducted during its development as an antidepressant and anxiolytic agent in the 1970s. The compound was evaluated in preclinical and clinical settings but was never commercially marketed. As an SNRI, it would be expected to increase synaptic monoamine levels and produce antidepressant-like effects in animal models. The compound's anticonvulsant activity suggests potential effects in seizure models. However, specific in vivo efficacy data and detailed animal model studies are limited in publicly available literature. The compound remains a research tool for studying monoamine reuptake inhibition and related neurological mechanisms.
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| Enzyme Assay |
For serotonin transporter binding assays, membrane preparations from cells expressing human recombinant SERT are incubated with radiolabeled ligands (e.g., [3H]-paroxetine or [3H]-citalopram) and varying concentrations of Clovoxamine. Non-specific binding is determined using excess unlabeled reference compound (e.g., fluoxetine). Following incubation at appropriate temperature (typically 4-25°C for 60-120 minutes), bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed, dried, and radioactivity counted by liquid scintillation. Ki values are calculated from competitive binding curves using the Cheng-Prusoff equation. Assays are performed in triplicate with appropriate vehicle controls.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing serotonin transporters (e.g., HEK293 or CHO cells transfected with SERT) are cultured in appropriate media under standard conditions (37°C, 5% CO2). Clovoxamine is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are seeded in multi-well plates and pre-incubated with test compound. Serotonin uptake is measured by adding radiolabeled [3H]-5-HT and quantifying intracellular radioactivity after washing. Alternatively, neurotransmitter levels can be measured by HPLC or LC-MS. For cell viability assays, standard MTT or CCK-8 assays can be used. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
For in vivo animal studies of Clovoxamine, no specific published protocols are available. As an SNRI developed in the 1970s, it would have been evaluated in standard antidepressant models such as the forced swim test, tail suspension test, or learned helplessness models in rodents. Compounds are typically formulated in suitable vehicles (e.g., saline or DMSO/PEG mixtures) and administered via oral gavage, intraperitoneal (i.p.) injection, or subcutaneous (s.c.) injection. Dosing regimens vary by study objective. For pharmacokinetic studies, blood and brain tissue samples are collected at predetermined time points. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Clovoxamine are characteristic of a small-molecule SNRI. The compound has a molecular weight of 284.78, formula C14H21ClN2O2, and CAS number 54739-19-4. The fumarate salt has a molecular weight of 400.856 and CAS number 54739-21-8. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Solubility: soluble in DMSO. Appearance: liquid. Purity: >98%. Specific pharmacokinetic parameters such as half-life, clearance, and oral bioavailability are not extensively reported in publicly available sources.
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| Toxicity/Toxicokinetics |
According to available safety information, Clovoxamine is intended for research use only and cannot be used to diagnose, treat or manage patients. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available as the compound was never commercially marketed.
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| References |
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| Additional Infomation |
Clovoxamine is a 5-methoxypentanone O-(2-aminoethyl) oxime, belonging to the monochlorobenzene class of compounds. It has antidepressant effects.
Clovoxamine (DU23811) is a non-tricyclic serotonin-norepinephrine reuptake inhibitor (SNRI) originally developed in the 1970s as an antidepressant and anxiolytic agent but never commercially marketed. It has binding affinity for SERT with a Ki of 61 nM and exhibits antidepressant and anticonvulsant activities. The compound has little affinity for muscarinic, histaminergic, serotonergic and adrenergic binding sites. It induces a decrease in beta-adrenergic receptor coupled c-AMP response. It is for research use only with no regulatory approvals reported. |
| Molecular Formula |
C14H21CLN2O2
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|---|---|
| Molecular Weight |
284.78
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| Exact Mass |
284.129
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| CAS # |
54739-19-4
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| PubChem CID |
6335903
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.12g/cm3
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| Boiling Point |
387.8ºC at 760 mmHg
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| Flash Point |
188.3ºC
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| Index of Refraction |
1.519
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| LogP |
3.536
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
19
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| Complexity |
254
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COCCCC/C(=N\OCCN)/c1ccc(cc1)ClCopyCopied
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| InChi Key |
XXPVSQRPGBUFKM-SAPNQHFASA-N
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| InChi Code |
InChI=1S/C14H21ClN2O2/c1-18-10-3-2-4-14(17-19-11-9-16)12-5-7-13(15)8-6-12/h5-8H,2-4,9-11,16H2,1H3/b17-14+
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| Chemical Name |
2-[(E)-[1-(4-chlorophenyl)-5-methoxypentylidene]amino]oxyethanamine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.5115 mL | 17.5574 mL | 35.1148 mL | |
| 5 mM | 0.7023 mL | 3.5115 mL | 7.0230 mL | |
| 10 mM | 0.3511 mL | 1.7557 mL | 3.5115 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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