| Bioactivity | 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)[1][2][3]. |
| Target | IC50: 3.6 nM (MAO-B), 680 nM (MAO-A) |
| Invitro | 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]. |
| 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]. Animal Model: |
| Name | Mofegiline hydrochloride |
| CAS | 120635-25-8 |
| Formula | C11H14ClF2N |
| Molar Mass | 233.69 |
| Appearance | Solid |
| Transport | 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) |
| Reference | [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]. 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. [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 [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. |
Mofegiline hydrochloride
CAS: 120635-25-8 F: C11H14ClF2N W: 233.69
Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B,
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