| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Mofegiline HCl (MDL-72,974; MDL72,974), the hydrochloride salt of Mofegiline, is a potent and irreversible inhibitor of monoamine oxidase B (MAO-B) and semicarbazide-sensitive amine oxidase (SSAO) with the potential to be used for the treatment for various diseases.
| ln Vitro |
Rat brain mitochondrial MAO is inhibited by murfegiline hydrochloride (MDL72974A) in a concentration- and time-dependent manner[1]. In the rat striatum, murfegiline hydrochloride (MDL72974A) has a poor effect[2] but reduces [3H]GBR-12935 (1 nM) binding (IC50 >100 μM) and [3H]dopamine (15 nM) uptake (IC50 of 31.8 μM). The aortas of dogs, rats, cows, and humans are all susceptible to SSAO inhibition by murfegiline hydrochloride (MDL72974A), with IC50 values of 2 nM, 5 nM, 80 nM, and 20 nM, respectively [3].
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| ln Vivo |
Murfegiline hydrochloride (MDL72974A) has the capacity to block MPTP in a mouse neurotoxicity model and inhibit MAO-B activity in vitro in a rat model (1.25 mg/kg; i.p.; 18 hours prior to MPTP treatment) [1].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (150-400 g)[1]
Doses: Group 1: 0.1-2.5 mg/kg; Group 2: 0.05-5 mg/kg Route of Administration: po (oral gavage); single dose for group 1, as for group 2, one time/day for 14 days Experimental Results:demonstrated 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/Disease Models: Mate SwissWebster (CF-W) mice (25-30 g)[1] Doses: 1.25 mg/kg Route of Administration: intraperitoneal (ip) injection; 18 hrs (hrs (hours)) prior to administration of MPTP (20 mg/kg; i.p.; 4 times for two-hourly intervals, for 8 days) Experimental Results:Rescued MPTP-induced decreases in striatal levels of dopamine (DA), dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in mice. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (150-400 g) injected with Tyramine (HY-W007606) (1.25-80 μg/kg; i.v.)[1] Doses: Group 1: 1.8, 9 mg/kg; Group 2: 0.1, 1 mg/kg Route of Administration: po (oral gavage); single dose for group 1, as for group 2, one time/day for 14 days Experimental Results:Did not Dramatically potentiate the cardiovascular effects of intraduodenally administered Tyramine (HY-W007606) in anaesthetised rats. |
| References |
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| Molecular Formula |
C11H14CLF2N
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|---|---|
| Molecular Weight |
233.6868
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| Exact Mass |
233.078
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| CAS # |
120635-25-8
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| PubChem CID |
6446650
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| Appearance |
White to off-white solid powder
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| Boiling Point |
322.7ºC at 760 mmHg
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| Flash Point |
149ºC
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| Vapour Pressure |
0.00232mmHg at 25°C
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| LogP |
4.072
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
184
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1CC/C(=C\F)/CN)F.Cl
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| InChi Key |
QUCNNQHLIHGBIA-HCUGZAAXSA-N
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| InChi Code |
InChI=1S/C11H13F2N.ClH/c12-7-10(8-14)2-1-9-3-5-11(13)6-4-9;/h3-7H,1-2,8,14H2;1H/b10-7+;
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| Chemical Name |
(2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine;hydrochloride
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| Synonyms |
MDL 72974A MDL72974A MDL-72974A
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~110 mg/mL (~470.71 mM)
H2O : ~25 mg/mL (~106.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (11.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (11.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (11.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (42.79 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*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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