| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
Iproniazid phosphate targets monoamine oxidase (MAO), an enzyme that catalyzes the oxidative deamination of monoamine neurotransmitters such as serotonin, norepinephrine, and dopamine. It is a non-selective and irreversible inhibitor of MAO, leading to increased levels of these neurotransmitters in the brain.
|
|---|---|
| ln Vitro |
Iproniazid phosphate inhibits MAO activity and enhances Rotenone-induced apoptosis. As a non-selective MAO inhibitor, it increases the levels of monoamine neurotransmitters such as serotonin, norepinephrine, and dopamine in the brain. The compound has antidepressive activity.
|
| ln Vivo |
Iproniazid phosphate has been studied in clinical settings as an antidepressant. However, its use was discontinued due to its potential for inducing liver toxicity. The compound has been used in research to study the effects of MAO inhibition on neurotransmitter metabolism and behavior.
|
| Enzyme Assay |
The in vitro enzyme inhibition assay for Iproniazid phosphate typically involves measuring its inhibitory activity against MAO using a standard enzyme assay. The compound is incubated with the enzyme and a substrate (e.g., serotonin, tyramine), and the production of the oxidative deamination product is measured. The IC50 value is determined from the dose-response curve.
|
| Cell Assay |
The in vitro cellular assay for Iproniazid phosphate typically involves culturing neuronal cells or other relevant cell types in appropriate growth media. Cells are treated with varying concentrations of the compound, and the levels of monoamine neurotransmitters or their metabolites are measured using HPLC or ELISA. The compound's effects on MAO activity and neurotransmitter metabolism are assessed.
|
| Animal Protocol |
In vivo animal studies for Iproniazid phosphate typically involve the administration of the compound to rodents via oral gavage or intraperitoneal injection. Behavioral tests such as the forced swim test or tail suspension test are used to assess antidepressant-like effects. Neurotransmitter levels in the brain are measured using microdialysis or tissue homogenate analysis.
|
| ADME/Pharmacokinetics |
Iproniazid phosphate has a molecular weight of 277.21 g/mol and a molecular formula of C9H16N3O5P. The melting point is 175-184°C. The IUPAC name is 4-Pyridinecarboxylic acid, 2-(1-methylethyl)hydrazide, phosphate (1:1). The compound is soluble in water and other solvents. Further detailed physicochemical properties are available from the manufacturer's data sheets.
|
| Toxicity/Toxicokinetics |
Iproniazid phosphate has been associated with liver toxicity, which led to the discontinuation of its use as an antidepressant. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling and disposal information.
|
| References | |
| Additional Infomation |
Iproniazid is a carbapenemhydrin compound belonging to the pyridine class. Due to interactions with tyrosine-containing foods, it was withdrawn from the Canadian market in July 1964. It is an irreversible monoamine oxidase A and B inhibitor used as an antidepressant. It was also used as an anti-tuberculosis drug, but its use was limited due to its toxicity. Drug Indications: For the treatment of depression (originally used to treat tuberculosis). Pharmacodynamics: Iproniazid is a monoamine oxidase inhibitor (MAOI) and was the first antidepressant developed.
Iproniazid phosphate (Marsilid, Iprazid) is a non-selective, irreversible monoamine oxidase (MAO) inhibitor (MAOI) of the hydrazine class. It was first synthesized in the 1950s and was initially developed as an antidepressant. Its use was discontinued due to its potential for inducing liver toxicity. The compound is used in research to study MAO inhibition. It is also known by the synonyms Marsilid phosphate, NSC 81850, and 1-Isonicotinyl-2-isopropylhydrazine phosphate. |
| Molecular Formula |
C9H13N3O.H3O4P
|
|---|---|
| Molecular Weight |
277.21424
|
| Exact Mass |
277.083
|
| CAS # |
305-33-9
|
| Related CAS # |
Iproniazid;54-92-2
|
| PubChem CID |
3748
|
| Appearance |
White to off-white solid powder
|
| Density |
1.084g/cm3
|
| Boiling Point |
265.9ºC at 760mmHg
|
| Melting Point |
181ºC
|
| Flash Point |
114.6ºC
|
| LogP |
0.577
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
13
|
| Complexity |
164
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NYMGNSNKLVNMIA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H13N3O/c1-7(2)11-12-9(13)8-3-5-10-6-4-8/h3-7,11H,1-2H3,(H,12,13)
|
| Chemical Name |
N'-propan-2-ylpyridine-4-carbohydrazide
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~360.74 mM)
H2O : ≥ 50 mg/mL (~180.37 mM) |
|---|---|
| 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 | 3.6074 mL | 18.0369 mL | 36.0737 mL | |
| 5 mM | 0.7215 mL | 3.6074 mL | 7.2147 mL | |
| 10 mM | 0.3607 mL | 1.8037 mL | 3.6074 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
