1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Mofegiline hydrochloride

Mofegiline hydrochloride  (Synonyms: MDL72974A)

Cat. No.: HY-16677A Purity: ≥95.0%
COA Handling Instructions

Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO).

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Mofegiline hydrochloride Chemical Structure

Mofegiline hydrochloride Chemical Structure

CAS No. : 120635-25-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 125 In-stock
Solution
10 mM * 1 mL in DMSO USD 125 In-stock
Solid
5 mg USD 114 In-stock
10 mg USD 168 In-stock
50 mg USD 504 In-stock
100 mg USD 754 In-stock
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Description

Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO)[1][2][3].

IC50 & Target

IC50: 3.6 nM (MAO-B), 680 nM (MAO-A)[1]

In Vitro

Mofegiline hydrochloride (MDL72974A) inhibits rat brain mitochondrial MAO in a concentration and time-dependent fashion[1].
Mofegiline hydrochloride (MDL72974A) inhibits [3H]dopamine (15 nM) uptake with an IC50 value of 31.8 μM, but poorly inhibits [3H]GBR-12935 (1 nM) binding (IC50 >100 μM) in the rat striatum[2].
Mofegiline hydrochloride (MDL72974A) inhibits SSAOs from dog aorta, rat aorta, bovine aorta and human umbilical artery with IC50s of 2 nM, 5 nM, 80 nM and 20 nM, respectively[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mofegiline hydrochloride (MDL72974A) (0.1-2.5 mg/kg; p.o.; single dose) inhibits MAO-B activity external vivo in rat model and (1.25 mg/kg; i.p.; 18 hours prior to MPTP treatment) exerts its ability to block MPTP neurotoxicity in mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (150-400 g)[1]
Dosage: Group 1: 0.1-2.5 mg/kg; Group 2: 0.05-5 mg/kg
Administration: Oral gavage; single dose for group 1, as for group 2, once daily for 14 days
Result: Showed the inhibition effect on rat brain MAO-A and MAO-B with EC50s of 8 mg/kg and 0.18 mg/kg, respectively, in group 1.
Resulted more potent efficacy on MAO-A inhibition in a daily dosed-manner (group 2) than single dose (group 1) manner, indicating a long half-life of Mofegiline hydrochloride.
Animal Model: Mate SwissWebster (CF-W) mice (25-30 g)[1]
Dosage: 1.25 mg/kg
Administration: Intraperitoneal injection; 18 hours prior to administration of MPTP (20 mg/kg; i.p.; 4 times for two-hourly intervals, for 8 days)
Result: Rescued MPTP-induced decreases in striatal levels of dopamine (DA), dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in mice.
Animal Model: Male Sprague-Dawley rats (150-400 g) injected with Tyramine (HY-W007606) (1.25-80 μg/kg; i.v.)[1]
Dosage: Group 1: 1.8, 9 mg/kg; Group 2: 0.1, 1 mg/kg
Administration: Oral gavage; single dose for group 1, as for group 2, once daily for 14 days
Result: Did not significantly potentiate the cardiovascular effects of intraduodenally administered Tyramine (HY-W007606) in anaesthetised rats.
Molecular Weight

233.69

Formula

C11H14ClF2N

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=C(CC/C(CN)=C(F)/[H])C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (470.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (106.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2792 mL 21.3959 mL 42.7917 mL
5 mM 0.8558 mL 4.2792 mL 8.5583 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.75 mg/mL (11.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (11.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 10 mg/mL (42.79 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.2792 mL 21.3959 mL 42.7917 mL 106.9793 mL
5 mM 0.8558 mL 4.2792 mL 8.5583 mL 21.3959 mL
10 mM 0.4279 mL 2.1396 mL 4.2792 mL 10.6979 mL
15 mM 0.2853 mL 1.4264 mL 2.8528 mL 7.1320 mL
20 mM 0.2140 mL 1.0698 mL 2.1396 mL 5.3490 mL
25 mM 0.1712 mL 0.8558 mL 1.7117 mL 4.2792 mL
30 mM 0.1426 mL 0.7132 mL 1.4264 mL 3.5660 mL
40 mM 0.1070 mL 0.5349 mL 1.0698 mL 2.6745 mL
50 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1396 mL
60 mM 0.0713 mL 0.3566 mL 0.7132 mL 1.7830 mL
80 mM 0.0535 mL 0.2674 mL 0.5349 mL 1.3372 mL
100 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mofegiline hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mofegiline hydrochloride
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