Mofegiline hydrochloride
(Synonyms: 盐酸莫非吉林; MDL72974A) 目录号 : GC36638
An inhibitor of MAO-B
Cas No.:120635-25-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mofegiline is an inhibitor of monoamine oxidase B (MAO-B; IC50 = 3.6 nM for the rat brain mitochondrial enzyme).1 It is selective for MAO-B over MAO-A (IC50 = 680 nM). Mofegiline also inhibits vascular adhesion protein-1 (VAP-1), also known as semicarbazide-sensitive amine oxidase (SSAO), an enzyme that has roles in leukocyte adhesion and transmigration, with an IC50 value of 20 nM for the human enzyme.2 It reduces MPTP-induced decreases in striatal levels of dopamine, dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) in mice when administered at a dose of 1.25 mg/kg.1 Mofegiline (5 mg/kg) also inhibits LPS-induced increases in bronchoalveolar lavage fluid (BALF) levels of TNF-α in transgenic mice overexpressing VAP-1.
1.Zreika, M., Fozard, J.R., Dudley, M.W., 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 diseaseJ. Neural Transm. Park. Dis. Dement. Sect.1(4)243-254(1989) 2.Foot, J.S., Deodhar, M., Turner, C.I., et al.The discovery and development of selective 3-fluoro-4-aryloxyallylamine inhibitors of the amine oxidase activity of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1)Bioorg. Med. Chem. Lett.22(12)3935-3940(2012)
| Cas No. | 120635-25-8 | SDF | |
| 别名 | 盐酸莫非吉林; MDL72974A | ||
| Canonical SMILES | FC1=CC=C(CC/C(CN)=C(F)/[H])C=C1.[H]Cl | ||
| 分子式 | C11H14ClF2N | 分子量 | 233.69 |
| 溶解度 | Water: ≥ 39 mg/mL (166.89 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.PMID:7835226doi
Mofegiline or MDL 72,974A ((E)-4-fluoro-beta-fluoromethylene benzene butanamine hydrochloride) is a selective enzyme-activated irreversible inhibitor of monoamine oxidase B, which is under development for use in the treatment of Parkinson's disease. 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. HPLC, with on-line radioactivity detection, showed the presence of four major peaks (M1, M2, M3, and M4), representing respectively 50, 9, 5, and 0.5% of the administered dose excreted in 0-24 hr urine. TSP-LC-MS, FAB-MS, and NMR spectra of the purified metabolites were obtained. M1, the major metabolite in dogs, was shown to have undergone defluorination of the beta-fluoromethylene moiety, and one carbon addition. Its structure was confirmed to be a cyclic carbamate. M2 was a N-carbamoyl O-beta-D-glucuronide conjugate of parent drug. The formation of M1 and M2 is likely to involve initial reversible addition of CO2 to the primary amine function. M3 was a N-succinyl conjugate of the parent drug. M4 had also undergone defluorination to yield a urea adduct of an unsaturated alpha, beta aldehyde. Structures of M1 and M3 were further confirmed by comparing their MS and NMR spectra with those of authentic reference compounds. TSP-LC-MS ion chromatograms of human urine, obtained from two male volunteers after p.o. administration of 24 mg of drug, showed selected molecular ion peaks with the same retention time as the metabolites identified in dogs. In humans, these common metabolites represented a similar percentage of the administered dose to that in dogs. The present study demonstrates that NMR, TSP-LC-MS are complementary analytical techniques, which allow structural identification of unhydrolyzed drug conjugates. The formation of carbamates of amine-containing drugs may be more common than previously reported.