产品
编 号：F070414
分子式：C11H14ClF2N
分子量：233.69
分子式：C11H14ClF2N
分子量：233.69
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 120635-25-8
产品详情
生物活性：
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).
体内研究：
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.Animal Model:Male Sprague-Dawley rats (150-400 g)
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)
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:Male Sprague-Dawley rats (150-400 g) injected with Tyramine (HY-W007606) (1.25-80 μg/kg; i.v.)
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.
体外研究：
Mofegiline hydrochloride (MDL72974A) inhibits rat brain mitochondrial MAO in a concentrationand time-dependent fashion.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.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.
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).
体内研究：
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.Animal Model:Male Sprague-Dawley rats (150-400 g)
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)
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:Male Sprague-Dawley rats (150-400 g) injected with Tyramine (HY-W007606) (1.25-80 μg/kg; i.v.)
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.
体外研究：
Mofegiline hydrochloride (MDL72974A) inhibits rat brain mitochondrial MAO in a concentrationand time-dependent fashion.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.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.
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