Mofegiline hydrochloride (Synonyms: 盐酸莫非吉林; MDL72974A)
目录号: PL07476 纯度: ≥95.0%
CAS No. :120635-25-8
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中文名称
Mofegiline hydrochloride
中文别名
莫非吉兰;盐酸莫非吉兰;盐酸莫非吉林
英文名称
Mofegiline hydrochloride
英文别名
(2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine,hydrochloride;Benzenebutanamine,4-fluoro-b-(fluoromethylene)-,hydrochloride (1:1), (bE)-;Mofegiline hydrochloride;(E)-1-amino-2-(fluoromethylene)-4-(p-fluorophenyl)butane hydrochloride salt;(E)-2-(p-fluorophenethyl)-3-fluoroallylamine hydrochloric acid;MDL 72974A;MDL-72974A;Mofegiline HCl;Mofegiline hydrochloride (USAN)
Cas No.
120635-25-8
分子式
C11H13NF2.HCl
分子量
233.69
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Mofegiline hydrochloride (MDL72974A) 是一种靶向 MAO-B,酶激活不可逆的抑制剂,具有口服活性和选择性。Mofegiline hydrochloride 对 MAO-A 和 MAO-B 的 IC50 分别为 680 nM 和 3.6 nM。Mofegiline hydrochloride 也是一种氨基脲敏感胺氧化酶 (SSAO) 的抑制剂。
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 IC 50 s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO).
性状
Solid
IC50 & Target[1][2]
IC50: 3.6 nM (MAO-B), 680 nM (MAO-A)
体外研究(In Vitro)
Mofegiline hydrochloride (MDL72974A) inhibits rat brain mitochondrial MAO in a concentration and time-dependent fashion.
Mofegiline hydrochloride (MDL72974A) inhibits [H]dopamine (15 nM) uptake with an IC50 value of 31.8 μM, but poorly inhibits [H]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.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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 Parkinsons 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. 
溶解度数据
In Vitro: DMSO : 110 mg/mL (470.71 mM; Need ultrasonic)H2O : 25 mg/mL (106.98 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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