Mofegiline hydrochloride
Based on 1 Customer Validation
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.
- Purity: 99.57%
- CAS No.: 120635-25-8
- Formula: C11H14ClF2N
- Molecular Weight:233.69
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Neuronal Signaling Compound Library
HY-L013
-
Reprogramming Compound Library
HY-L039
-
Orally Active Compound Library
HY-L061
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Mitochondria-Targeted Compound Library
HY-L089
-
Antidepressant Compound Library
HY-L108
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
MCE Bioactive Compound Library
HY-L001V
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
IC50: 3.6 nM (MAO-B), 680 nM (MAO-A)[1]
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.
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:
-
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.
Chemical Information
-
CAS No. 120635-25-8
-
Appearance Solid
-
Molecular Weight 233.69
-
Formula C11H14ClF2N
-
Color White to off-white
-
SMILES
FC1=CC=C(CC/C(CN)=C(F)/[H])C=C1.[H]Cl
-
Synonyms
MDL72974A
-
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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 10 mg/mL (42.79 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 Jan 22;43(2):307-12. [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
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.
Mofegiline hydrochloride Related Classifications
HY-16677A Related Classifications
Powered by Bioz