| Company Name: |
Beijing Boorsen Biotechnology Co., Ltd
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| Tel: |
400-901-9800 18611424007 |
| Email: |
cis@bioss.com.cn |
| Products Intro: |
Product Name:(2R)-1-(tert-butylamino)-3-{[4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl]oxy}propan-2-ol; but-2-enedioic acid
Purity:0.95 Package:1mg;1mL x 10mM (in DMSO) Remarks:D56068
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| | but-2-enedioic acid Basic information |
| Product Name: | but-2-enedioic acid | | Synonyms: | but-2-enedioic acid;1-Propanone, 3-(1-(phenylmethyl)-4-piperidinyl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)-,(E)-2-butenedioate (1:1);{2-[(4-chlorophenyl)(pyridin-2-yl)methoxy]ethyl}dimethylamine, 1 g;{2-[(4-chlorophenyl)(pyridin-2-yl)methoxy]ethyl}dimethylamine, 250 mg | | CAS: | 142852-51-5 | | MF: | C25H32N2O.C4H4O4 | | MW: | 492.61 | | EINECS: | | | Product Categories: | | | Mol File: | 142852-51-5.mol |  |
| | but-2-enedioic acid Chemical Properties |
| form | Solid | | color | White to off-white |
| | but-2-enedioic acid Usage And Synthesis |
| Uses | Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD)[1][2]. | | Definition | ChEBI: Zanapezil fumarate is a polymer. | | in vivo | Oral administration of Zanapezil (TAK-147; 3 mg/kg) significantly accelerated the turnover rates of dopamine, noradrenaline and serotonin in the rat brain. Oral administration of Zanapezil at doses ranging from 1 to 10 mg/kg induces a statistically significant and dose-dependent decrease in AChE activity in the cerebral cortex in ex vivo experiments[1].
Zanapezil (TAK-147; 5 and 10 mg/kg) significantly increases ACh level in the ventral hippocampus (VH) for 120 min[2]. | | IC 50 | AChE | | References | [1] K Hirai, et al. Neurochemical effects of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-b enzazepin-8-yl)-1-propanone fumarate (TAK-147), a novel acetylcholinesterase inhibitor, in rats. J Pharmacol Exp Ther. 1997 Mar;280(3):1261-9. PMID:9067312
[2] Izzettin Hatip-Al-Khatib,et al. Comparison of the effect of TAK-147 (zanapezil) and E-2020 (donepezil) on extracellular acetylcholine level and blood flow in the ventral hippocampus of freely moving rats. Brain Res. 2004 Jun 25;1012(1-2):169-76. DOI:10.1016/j.brainres.2004.03.067 |
| | but-2-enedioic acid Preparation Products And Raw materials |
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