Mofegiline hydrochloride

CAS# 120635-25-8

Mofegiline hydrochloride

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Mofegiline hydrochloride

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Chemical Properties of Mofegiline hydrochloride

Cas No. 120635-25-8 SDF Download SDF
PubChem ID 6446650 Appearance Powder
Formula C11H14ClF2N M.Wt 233.69
Type of Compound N/A Storage Desiccate at -20°C
Synonyms MDL72974A
Solubility H2O : ≥ 39 mg/mL (166.89 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine;hydrochloride
SMILES C1=CC(=CC=C1CCC(=CF)CN)F.Cl
Standard InChIKey QUCNNQHLIHGBIA-HCUGZAAXSA-N
Standard InChI 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+;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Mofegiline hydrochloride Dilution Calculator

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Mofegiline hydrochloride Molarity Calculator

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Preparing Stock Solutions of Mofegiline hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.2792 mL 21.3959 mL 42.7917 mL 85.5835 mL 106.9793 mL
5 mM 0.8558 mL 4.2792 mL 8.5583 mL 17.1167 mL 21.3959 mL
10 mM 0.4279 mL 2.1396 mL 4.2792 mL 8.5583 mL 10.6979 mL
50 mM 0.0856 mL 0.4279 mL 0.8558 mL 1.7117 mL 2.1396 mL
100 mM 0.0428 mL 0.214 mL 0.4279 mL 0.8558 mL 1.0698 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Mofegiline hydrochloride

Mofegiline Hcl (MDL72974A) is a potent and selective enzyme-activated irreversible inhibitor of MAO-B; shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B). IC50 value: 3.6 nM [1] Target: MAO-B in vitro: MDL72974 inhibits rat brain mitochondrial MAO in a concentration and time-dependent fashion and shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B, respectively) [1]. is also capable of inhibiting semicarbazide-sensitive amine oxidases (SSAOs) obtained from vascular tissues and sera of different species. The inhibition of SSAO by MDL-72974A was irreversible and time dependent. It was competitive without preincubation of the enzyme with the inhibitor and demonstrated a mixed-type of inhibition when the enzyme was preincubated with the inhibitor. The IC50 values were estimated to be 2 x 10(-9) M, 5 x 10(-9) M, 8 x 10(-8) M and 2 x 10(-8) M for SSAO from dog aorta, rat aorta, bovine aorta and human umbilical artery, respectively [2]. in vivo: After oral administration to rats, the compound shows preferential inhibition of brain MAO-B with ED50 values of 8 and 0.18 mg/kg p.o. for the A and B forms, respectively. Selectivity is retained on repeat dosing. MDL 72,974 did not significantly potentiate the cardiovascular effects of intraduodenually-administered tyramine in anaesthetized rats and had only minor indirect sympathomimatic effects in the pithed rat [1]. Male beagle dogs were given single p.o. (20 mg/kg) and i.v. (5 mg/kg) doses of [14C]-Mofegiline. Total radioactivity excreted in urine and feces over 96 hr was, respectively, 75.5 +/- 3.8 and 6.3 +/- 3.4% of the dose after p.o. and 67.9 +/- 0.5 and 3.9 +/- 2.4% after i.v. administration. Unchanged drug in urine represented 3% of the dose after po and less than 1% after i.v. administration. Mofegiline was thus extensively metabolized in dogs, and urinary excretion was the major route of elimination of metabolites [3].

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. [2]. 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 [3]. 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.

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Mofegiline hydrochloride (MDL72974A) is a potent and selective enzyme-activated irreversible inhibitor of MAO-B; shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B).

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