PeptideDB

MAO-B-IN-4

MAO-B-IN-4

CAS No.:

MAO-B-IN-4 (Compound 26) is an orally bioactive, reversible inhibitor of MAO-B with IC50 of 9 nM. MAO-B-IN-4 has good me
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

MAO-B-IN-4 (Compound 26) is an orally bioactive, reversible inhibitor of MAO-B with IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety and can penetrate the BBB (blood-brain barrier). MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 has glial protective effects on astrocytes. MAO-B-IN-4 could be used in research related to AD/Alzheimer's disease.

Physicochemical Properties


Molecular Formula C23H20CLF2N3
Molecular Weight 411.87
Appearance Typically exists as solid at room temperature
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)

Biological Activity


ln Vitro In a model of cultured astrocytes, MAO-B-IN-4 (0.25 μM exposed to 0.5 μM DOX for 24 hours) demonstrated considerable glial protection [1].
ln Vivo MAO-B-IN-4 (1 and 3 mg/kg, orally, for 2 hours) guards against short-term memory impairment brought on by scopolamine [1]. In the forced swimming test, mice treated with MAO-B-IN-4 (0.312-2.5 mg/kg, intravenous injection, 1 hour) show antidepressant effects [1].
Cell Assay Cell Viability Assay[1]
Cell Types: HepG2 cells
Tested Concentrations: 0.1-100 µM
Incubation Duration: 72 h
Experimental Results: demonstrated no effect on the viability of the cells after 24 hrs (hours) of exposure.
Animal Protocol Animal/Disease Models: Rats treated with anticholinergic scopolamine[1]
Doses: 1 and 3 mg/kg
Route of Administration: Oral administration; 2h before the experiment
Experimental Results: Orally 2 h before the trial acquisition prevented scopolamine-induced short-term memory deficits Animal/Disease Models: Mice models[1]p>
Doses: 0.312-2.5 mg/kg
Route of Administration: intraperitoneal (ip)injection; 1h
Experimental Results: Resulted a similar effect with antidepressant S-citalopram (HY-14258) under the dose of 0.625 mg/kg and 1.25 mg/kg, accordingly.
References

[1]. Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines. Eur J Med Chem. 2022 Jun 5;236:114329.


Solubility Data


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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4280 mL 12.1398 mL 24.2795 mL
5 mM 0.4856 mL 2.4280 mL 4.8559 mL
10 mM 0.2428 mL 1.2140 mL 2.4280 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.