| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MAO-A 37 nM (IC50) MAO-B 57 nM (IC50)
MAO-IN-M30 dihydrochloride targets monoamine oxidase enzymes, specifically both the MAO-A and MAO-B isoforms. These are key enzymes in the brain responsible for the oxidative deamination of neurotransmitters like serotonin, dopamine, and norepinephrine. By irreversibly inhibiting both isoforms, it increases the levels of these monoamines in the synaptic cleft, which is a mechanism relevant to neurodegenerative and psychiatric disorders. |
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| ln Vitro |
After being exposed to dexamethasone for 72 hours, MAO-IN-M30 (0.25 nM) dramatically enhanced cell viability to approximately 90%[3]. Over a 24-hour period, MAO-IN-M30 (0–10 μM) improves PC12 cell survival[4]. In SH-SY5Y cells, MAO-IN-M30 therapy dramatically reduces the incidence of fragmented DNA when compared to the dexamethasone-treated group[3].
In vitro, MAO-IN-M30 dihydrochloride (0.25 nM, 72 hours) significantly increased cell viability to approximately 90% in SH-SY5Y cells after exposure to dexamethasone-induced apoptosis. It also enhanced PC12 cell survival at concentrations of 0-10 μM over 24 hours. Treatment with the compound significantly decreased the occurrence of fragmented DNA compared to the dexamethasone-treated group in SH-SY5Y cells, confirming its neuroprotective effect. |
| ln Vivo |
Neuroprotective properties are exhibited by MAO-IN-M30 (0.5-2.5 mg/kg; po; once daily for 14 consecutive days)[6].
In vivo, MAO-IN-M30 dihydrochloride (0.5-2.5 mg/kg; p.o.; once daily for 14 consecutive days) possesses neuroprotective activities. It has demonstrated neuro-restorative activity in MPTP and lactacystin models of Parkinson's disease. The compound's ability to cross the blood-brain barrier and its multifunctional mechanism (MAO inhibition, iron chelation, and radical scavenging) contribute to its efficacy in these models. |
| Enzyme Assay |
Non-cell-based enzyme assays are used to evaluate MAO-IN-M30 dihydrochloride's inhibitory activity against MAO-A and MAO-B. The compound is incubated with the respective enzyme and a suitable substrate, such as kynuramine. The production of the fluorescent metabolite, 4-hydroxyquinoline, is measured to determine enzyme activity. IC50 values are calculated from inhibition curves by plotting inhibitor concentration against residual enzyme activity and using non-linear regression analysis.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: SH-SY5Y cells Tested Concentrations: 0.25 nM Incubation Duration: 72 hrs (hours) Experimental Results: Dramatically increased cell viability to ∼90% after exposure to Dexamethasone. Cell Viability Assay[4] Cell Types: PC12 cells Tested Concentrations: 0-10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Enhanced the PC12 cell viability, the cell viability increasing to 85 ± 6 and 90 ± 7%. For in vitro cellular assays, cell lines like SH-SY5Y and PC12 are cultured in appropriate media. Cells are pre-incubated with various concentrations of MAO-IN-M30 dihydrochloride for a set period (e.g., 24-72 hours). To induce apoptosis, cells may be exposed to dexamethasone. Cell viability is then assessed using assays such as MTT or by measuring DNA fragmentation. The protective effect of the compound is determined by comparing cell viability in treated versus untreated control groups. |
| Animal Protocol |
Animal/Disease Models: Male C57/BL mice (20-22 g; MPTP-induced neurotoxicity in mice)[6]
Doses: 0.5, 2.5 mg/kg Route of Administration: Po; one time/day for 14 days Experimental Results: Dramatically elevate striatal dopamine levels, reduce its metabolism, and elevate tyrosine-hydroxylase protein levels and activity. Elevated MPTP-decreased dopaminergic and transferrin receptor cell count in the SNpc. For in vivo animal studies, MAO-IN-M30 dihydrochloride is typically administered orally to rodents (e.g., mice). In the MPTP Parkinson's disease model, the compound is given once daily for 14 consecutive days at doses ranging from 0.5 to 2.5 mg/kg. Following treatment, neuroprotective and neurorestorative effects are assessed by evaluating behavioral outcomes and histopathological markers of dopaminergic neuron survival in the brain. |
| ADME/Pharmacokinetics |
MAO-IN-M30 dihydrochloride is an orally active compound that can cross the blood-brain barrier. Its molecular weight is 299.2 g/mol. For in vitro use, it is soluble in DMSO (2 mg/mL) with ultrasonic and warming assistance. Stock solutions should be stored at -80°C for up to 6 months or at -20°C for up to 1 month, sealed and away from moisture. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of MAO-IN-M30 dihydrochloride is not extensively detailed in the provided literature. As with other MAO inhibitors, potential adverse effects could include those related to increased monoamine levels. However, the compound is noted for its neuroprotective properties against dexamethasone-induced apoptosis. It is for research use only and should be handled with standard laboratory safety precautions.
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| References |
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| Additional Infomation |
MAO-IN-M30 dihydrochloride (CAS#: 64821-19-8) is a multifunctional, brain-selective MAO-A/B inhibitor. Its mechanism of action is based on irreversible inhibition of MAO enzymes, combined with iron-chelating and free radical-scavenging activities. This multi-target profile is designed to provide neuroprotection. It has been studied in models of Parkinson's disease and is used as a research tool in neurodegenerative disease research. It has not been approved for clinical use.
|
| Molecular Formula |
C14H16CL2N2O
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|---|---|
| Molecular Weight |
299.20
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| Exact Mass |
298.064
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| CAS # |
64821-19-8
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| PubChem CID |
71311622
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| Appearance |
White to yellow solid powder
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| LogP |
3.609
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
|
| Heavy Atom Count |
19
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| Complexity |
296
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(CC#C)CC1=C2C=CC=NC2=C(C=C1)O.Cl.Cl
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| InChi Key |
XJNICPXVRPOSSO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14N2O.2ClH/c1-3-9-16(2)10-11-6-7-13(17)14-12(11)5-4-8-15-14;;/h1,4-8,17H,9-10H2,2H3;2*1H
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| Chemical Name |
5-[[methyl(prop-2-ynyl)amino]methyl]quinolin-8-ol;dihydrochloride
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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, 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)
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| Solubility (In Vitro) |
DMSO: 2 mg/mL (6.68 mM)
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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 | 3.3422 mL | 16.7112 mL | 33.4225 mL | |
| 5 mM | 0.6684 mL | 3.3422 mL | 6.6845 mL | |
| 10 mM | 0.3342 mL | 1.6711 mL | 3.3422 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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