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

Mofegiline hydrochloride (Synonyms: MDL72974A)

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

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).

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

Mofegiline hydrochloride Chemical Structure

Mofegiline hydrochloride Chemical Structure

CAS No. : 120635-25-8

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10 mM * 1  mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
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10 mg USD 168 In-stock
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50 mg USD 504 In-stock
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100 mg USD 754 In-stock
Estimated Time of Arrival: December 31
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Description

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). 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].

Molecular Weight

233.69

Formula

C₁₁H₁₄ClF₂N

CAS No.

120635-25-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (470.71 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

MofegilineMDL72974AMonoamine OxidaseMAOInhibitorinhibitorinhibit

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Mofegiline hydrochloride
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HY-16677A
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