| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Amiflamine targets monoamine oxidase A (MAO-A), a mitochondrial enzyme that catalyzes the oxidative deamination of monoamine neurotransmitters including serotonin, norepinephrine, and dopamine. It acts as a selective and reversible inhibitor of MAO-A. By inhibiting MAO-A, amiflamine increases the concentration of these neurotransmitters in the synaptic cleft, enhancing monoaminergic neurotransmission. This mechanism is similar to that of other MAO inhibitors used in the treatment of depression. Its selectivity for MAO-A over MAO-B distinguishes it from non-selective MAO inhibitors.
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|---|---|
| ln Vitro |
Amiflamine demonstrates potent in vitro activity as a MAO-A inhibitor. In enzyme assays using MAO-A purified from tissues or cells, amiflamine inhibits the oxidation of MAO-A substrates such as serotonin or tyramine in a concentration-dependent manner. Its IC50 for MAO-A inhibition is in the nanomolar to micromolar range. The compound shows selectivity for MAO-A over MAO-B, which is important for avoiding the dietary tyramine interactions associated with non-selective MAO inhibitors. Its reversible inhibition distinguishes it from irreversible MAO inhibitors.
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| ln Vivo |
Amiflamine demonstrates in vivo activity as a MAO-A inhibitor. In animal models, it increases brain levels of serotonin, norepinephrine, and dopamine. As a short-acting MAO-A inhibitor, it would be expected to produce acute effects on monoamine levels. It was investigated as a potential antidepressant but was not developed clinically. Its in vivo effects are dose-dependent and reversible, consistent with its mechanism as a reversible MAO-A inhibitor. The compound may also affect behavior in animal models of depression.
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| Enzyme Assay |
The in vitro enzyme assay for amiflamine measures its inhibition of MAO-A activity. MAO-A enzyme (purified from human placenta or recombinant) is incubated with a substrate (e.g., serotonin, tyramine, or kynuramine) and varying concentrations of amiflamine in appropriate buffer at 37°C. The oxidation of the substrate is measured by spectrophotometric detection of the reaction product (e.g., 4-hydroxyquinoline from kynuramine). IC50 values are calculated from dose-response curves using non-linear regression. Selectivity for MAO-A over MAO-B is assessed by testing against MAO-B using a MAO-B-specific substrate (e.g., benzylamine).
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| Cell Assay |
In vitro cellular assays for amiflamine are performed using cell lines expressing MAO-A, such as neuroblastoma cells (SH-SY5Y) or MAO-A-transfected HEK-293 cells. Cells are cultured in appropriate medium and treated with varying concentrations of amiflamine (typically 0.01-100 μM). Cellular MAO-A activity is measured by incubating cell lysates or intact cells with a MAO-A substrate and detecting the oxidation product by fluorescence or absorbance. The increase in neurotransmitter levels in the culture medium can be measured by ELISA or HPLC. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal experiments for amiflamine are conducted in rodent models. Amiflamine is formulated in appropriate vehicle and administered via intraperitoneal or oral administration at various doses (typically 0.1-10 mg/kg). Brain tissue is harvested at various time points after administration. Monoamine levels (serotonin, norepinephrine, dopamine) and their metabolites are measured in brain homogenates by HPLC with electrochemical detection. MAO-A activity in brain tissue is measured ex vivo using a fluorogenic substrate. Behavioral tests such as the forced swim test may be used to assess antidepressant-like effects. Pharmacokinetic parameters are determined from plasma samples.
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| References |
| Molecular Formula |
C12H20N2
|
|---|---|
| Molecular Weight |
192.3006
|
| Exact Mass |
192.163
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| CAS # |
77518-07-1
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| PubChem CID |
71221
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| Appearance |
Typically exists as solid at room temperature
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| Density |
0.975g/cm3
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| Boiling Point |
313ºC at 760 mmHg
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| Flash Point |
130.3ºC
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| Index of Refraction |
1.553
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| LogP |
2.651
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| tPSA |
29.26
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
168
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
C[C@@H](CC1C=CC(N(C)C)=CC=1C)N
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| InChi Key |
HFQMYSHATTXRTC-JTQLQIEISA-N
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| InChi Code |
InChI=1S/C12H20N2/c1-9-7-12(14(3)4)6-5-11(9)8-10(2)13/h5-7,10H,8,13H2,1-4H3/t10-/m0/s1
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| Chemical Name |
4-[(2S)-2-aminopropyl]-N,N,3-trimethylaniline
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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 | 5.2002 mL | 26.0010 mL | 52.0021 mL | |
| 5 mM | 1.0400 mL | 5.2002 mL | 10.4004 mL | |
| 10 mM | 0.5200 mL | 2.6001 mL | 5.2002 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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