| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Imipramine N-oxide does not have a specific therapeutic target but functions as a metabolite of imipramine and a substrate for flavin-containing monooxygenase (FMO) enzymes. FMO enzymes catalyze the N-oxidation of tertiary amines, and imipramine N-oxide is a product of this reaction. The compound may also interact with various transporters and enzymes involved in drug metabolism and disposition. It is studied for its role in the metabolism and pharmacokinetics of imipramine.
|
|---|---|
| ln Vitro |
Imipramine N-oxide is a metabolite of the tricyclic antidepressant imipramine. As an N-oxidized derivative, it exhibits interesting properties as a substrate for flavin-containing monooxygenase (FMO), where its oxidation alters its electronic structure, enhancing its solubility and reactivity. The compound has been investigated in clinical trials for potential therapeutic applications. Its biological activity is primarily related to its role in drug metabolism.
|
| ln Vivo |
In vivo, imipramine N-oxide is a circulating metabolite formed from the N-oxidation of imipramine. It is produced primarily by flavin-containing monooxygenases in the liver and other tissues. The compound may contribute to the pharmacological and toxicological effects of imipramine. It has been investigated in clinical trials, reaching a maximum phase of II. Specific in vivo efficacy studies for imipramine N-oxide as a standalone agent are not documented.
|
| Enzyme Assay |
The in vitro enzyme assay for imipramine N-oxide typically involves its use as a substrate for flavin-containing monooxygenase (FMO) enzymes. FMO enzymes are incubated with varying concentrations of imipramine (the parent compound) and NADPH, and the formation of imipramine N-oxide is measured by HPLC or LC-MS. The compound can also be used as a standard for the quantification of imipramine metabolites. The compound is dissolved in appropriate solvents such as methanol or DMSO.
|
| Cell Assay |
In vitro cellular assays for imipramine N-oxide typically involve treating cells expressing FMO enzymes with imipramine and measuring the formation of imipramine N-oxide. Cells are incubated with imipramine at concentrations ranging from 1 to 100 µM for various time periods. The metabolite is extracted and analyzed by HPLC or LC-MS. The compound's effects on cellular function are assessed using standard cell viability assays. The compound is dissolved in DMSO and diluted in cell culture medium.
|
| Animal Protocol |
In vivo animal studies for imipramine N-oxide are not typically performed for therapeutic purposes. The compound may be used in pharmacokinetic studies to assess imipramine metabolism in animal models. The compound is administered to animals, and blood, urine, and tissue samples are collected for analysis by mass spectrometry. The compound is not intended for human therapeutic use as a standalone agent. Standard metabolic studies would involve administration of imipramine and analysis of metabolites.
|
| ADME/Pharmacokinetics |
Imipramine N-oxide has a molecular weight of 296.41 g/mol and formula C19H24N2O. The compound is a highly polar, tertiary amine-oxidized derivative. Purity is typically ≥98%. Recommended storage is at room temperature or -20°C. The compound is soluble in DMSO and other organic solvents. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would be similar to other imipramine metabolites.
|
| Toxicity/Toxicokinetics |
Imipramine N-oxide is intended for research use only and is not approved for human therapeutic applications. As a metabolite of imipramine, it is generally considered to have low toxicity, but appropriate safety precautions should be taken when handling. The compound has been investigated in clinical trials, reaching a maximum phase of II. Standard toxicity assessments would include acute toxicity and repeated-dose toxicity studies if required.
|
| References | |
| Additional Infomation |
Imipramine oxide is a dibenzoxazole compound.
Imipramine N-oxide (CAS 6829-98-7) is a highly polar, tertiary amine-oxidized derivative and a circulating metabolite of the tricyclic antidepressant imipramine. It has a molecular weight of 296.41 g/mol and formula C19H24N2O. The compound is a dibenzooxazepine and has reached a maximum clinical trial phase of II. Imipramine N-oxide is used as a substrate for flavin-containing monooxygenase (FMO) enzymes. It is also known as imipraminoxide and IMIPRAMINE OXIDE. |
| Molecular Formula |
C19H24N2O
|
|---|---|
| Molecular Weight |
296.40666
|
| Exact Mass |
296.189
|
| CAS # |
6829-98-7
|
| Related CAS # |
19864-71-2 (hydrochloride);20438-98-6 (hydrochloride salt/solvate)
|
| PubChem CID |
65589
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
93-95ºC
|
| LogP |
3.973
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
22
|
| Complexity |
333
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
QZIQORUGXBPDSU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H24N2O/c1-21(2,22)15-7-14-20-18-10-5-3-8-16(18)12-13-17-9-4-6-11-19(17)20/h3-6,8-11H,7,12-15H2,1-2H3
|
| Chemical Name |
3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine oxide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~337.37 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.43 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (8.43 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 25.0 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: ≥ 2.5 mg/mL (8.43 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 | 3.3737 mL | 16.8685 mL | 33.7371 mL | |
| 5 mM | 0.6747 mL | 3.3737 mL | 6.7474 mL | |
| 10 mM | 0.3374 mL | 1.6869 mL | 3.3737 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
