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| Targets |
MAO-B-IN-8 targets monoamine oxidase B (MAO-B), an enzyme responsible for the oxidative deamination of biogenic and xenobiotic amines. MAO-B is primarily found in the brain and peripheral tissues and is a key therapeutic target for neurodegenerative diseases. By inhibiting MAO-B, the compound may help modulate neurotransmitter levels and reduce oxidative stress, which are implicated in the pathology of conditions like Parkinson's disease.
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| ln Vitro |
MAO-B-IN-8 is a potent reversible inhibitor of MAO-B. It also functions as an inhibitor of microglial production of neuroinflammatory mediators. The compound demonstrates high potency, with an IC50 value of 0.183 µM and a Ki of 0.094 µM. It is cell-permeable and inhibits HeLa cell growth with a GI50 of 2.7 µM. By inhibiting MAO-B and reducing neuroinflammation, it shows potential for neurodegenerative disease research.
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| ln Vivo |
In vivo activity data for MAO-B-IN-8 are not extensively detailed in the available literature. As a potent and reversible MAO-B inhibitor with additional neuroinflammatory mediator inhibitory effects, it is expected to exhibit neuroprotective activity in animal models of neurodegenerative diseases. The compound's specificity for MAO-B and its ability to cross the blood-brain barrier would be key factors for its in vivo efficacy. Specific dosing regimens and efficacy data would be determined from preclinical studies.
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| Enzyme Assay |
The in vitro enzyme assay for MAO-B-IN-8 typically involves measuring the inhibition of MAO-B enzymatic activity. Recombinant MAO-B enzyme is incubated with varying concentrations of the compound (typically 0.001-100 µM) in the presence of a substrate such as kynuramine or benzylamine. The enzymatic activity is measured by monitoring the production of the oxidized product (e.g., 4-hydroxyquinoline from kynuramine) using fluorescence or spectrophotometric methods. The IC50 value is determined by plotting the percentage of inhibition against compound concentration.
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| Cell Assay |
In vitro cellular assays for MAO-B-IN-8 typically involve treating microglial cells or neuronal cell lines with the compound at concentrations ranging from 0.001 to 10 µM for 24-72 hours. The inhibition of microglial production of neuroinflammatory mediators is assessed by measuring the levels of pro-inflammatory cytokines (such as TNF-α, IL-6, and IL-1β) in the culture supernatant using ELISA. Cell viability is assessed using MTT or CellTiter-Glo assays. The compound is dissolved in DMSO and diluted in cell culture medium.
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| Animal Protocol |
In vivo animal studies for MAO-B-IN-8 would typically involve administration to mice or rats via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Neurodegenerative disease models (such as MPTP-induced Parkinson's disease models) could be used to evaluate neuroprotective efficacy. Behavioral tests (such as locomotor activity and motor coordination) are performed to assess functional outcomes. Brain tissue is collected for biochemical analysis of MAO-B activity, oxidative stress markers, and neuroinflammatory mediators.
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| ADME/Pharmacokinetics |
MAO-B-IN-8 has a molecular weight of 328.32 g/mol and formula C18H16O6. It is highly soluble in DMSO at 112.5 mg/mL (342.7 mM). Recommended storage is powder at -20°C for up to 3 years and in solvent at -80°C for up to 1 year. The compound has high purity (99.62%) and appears as a red solid. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
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| Toxicity/Toxicokinetics |
MAO-B-IN-8 is intended for research use only and is not approved for human therapeutic applications. As a MAO-B inhibitor, it may affect normal neurotransmitter metabolism, which could contribute to potential side effects. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. The compound's inhibition of microglial neuroinflammatory mediators suggests it may have immunomodulatory effects.
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| References | |
| Additional Infomation |
MAO-B-IN-8 (CAS 1638956-60-1) is a potent reversible MAO-B inhibitor with a molecular weight of 328.32 g/mol and formula C18H16O6. It also inhibits microglial production of neuroinflammatory mediators. The compound is designed for neurodegenerative disease research, particularly for Parkinson's disease. Its mechanism of action involves inhibition of MAO-B enzymatic activity and reduction of neuroinflammation. MAO-B-IN-8 is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C18H16O6
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| Molecular Weight |
328.316045761108
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| Exact Mass |
328.094
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| CAS # |
1638956-60-1
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| PubChem CID |
667731
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C2=CC(O)=CC=C2C(=O)/C/1=C/C1=CC=C(OC)C(OC)=C1OC
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| InChi Key |
JGOPTESGPYJSBC-NVNXTCNLSA-N
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| InChi Code |
InChI=1S/C18H16O6/c1-21-13-7-4-10(17(22-2)18(13)23-3)8-15-16(20)12-6-5-11(19)9-14(12)24-15/h4-9,19H,1-3H3/b15-8-
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| Chemical Name |
(2Z)-6-hydroxy-2-[(2,3,4-trimethoxyphenyl)methylidene]-1-benzofuran-3-one
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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) |
DMSO : ~125 mg/mL (~380.73 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 | 3.0458 mL | 15.2290 mL | 30.4581 mL | |
| 5 mM | 0.6092 mL | 3.0458 mL | 6.0916 mL | |
| 10 mM | 0.3046 mL | 1.5229 mL | 3.0458 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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