Mofegiline hydrochloride (Synonyms: MDL72974A)

Cat. No.: HY-16677A Purity: 99.57%: FAQs
Data Sheet SDS COA Handling Instructions

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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).

For research use only. We do not sell to patients.

Mofegiline hydrochloride Chemical Structure

CAS No. : 120635-25-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 125	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 125	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 114	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 168	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 504	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 754	In-stock	Estimated Time of Arrival: December 31
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MAO-A MAO-B

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

120635-25-8

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
10 mM	0.4279 mL	2.1396 mL	4.2792 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (11.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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

Purity: 99.57%

Select Batch:

Data Sheet (276 KB) SDS (394 KB)

COA (245 KB) HNMR (256 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Zreika M, et al. MDL 72,974: a potent and selective enzyme-activated irreversible inhibitor of monoamine oxidase type B with potential for use in Parkinson's disease. J Neural Transm Park Dis Dement Sect. 1989;1(4):243-54. [Content Brief]

[2]. Fang J, et al. Effect of L-deprenyl, its structural analogues and some monoamine oxidase inhibitors on dopamine uptake. Neuropharmacology. 1994 Jun;33(6):763-8. [Content Brief]

[3]. Yu PH, et al. Inhibition of a type B monoamine oxidase inhibitor, (E)-2-(4-fluorophenethyl)-3-fluoroallylamine (MDL-72974A), on semicarbazide-sensitive amine oxidases isolated from vascular tissues and sera of different species. Biochem Pharmacol. 1992 Ja [Content Brief]

[4]. Dow J, et al. Novel carbamate metabolites of mofegiline, a primary amine monoamine oxidase B inhibitor, in dogs and humans. Drug Metab Dispos. 1994 Sep-Oct;22(5):738-49. [Content Brief]

Complete Stock Solution Preparation Table

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.

Mofegiline hydrochloride Related Classifications

Neurological Disease

Help & FAQs

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.

Keywords:

Mofegiline120635-25-8MDL72974AMonoamine OxidaseMAOenzyme-activatedirreversibleselectivityParkinson's diseasecardiovascular responsessemicarbazide-sensitive amine oxidasesdog aortarat aortabovine aorta and human umbilical arteryInhibitorinhibitorinhibit

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