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Rasagiline Mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rasagiline Mesylate图片
CAS NO:161735-79-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Rasagiline (R-AGN1135) mesylate 是一种高效的选择性不可逆线粒体单胺氧化酶 (MAO) 抑制剂,对大鼠脑 MAO B 和 A 活性的 IC50 分别为 4.43 nM 和 412 nM。
Cas No.161735-79-1
别名甲磺酸雷沙吉兰; (R)-AGN1135 mesylate; TVP1012 mesylate
化学名methanesulfonic acid;(1R)-N-prop-2-ynyl-2,3-dihydro-1H-inden-1-amine
Canonical SMILESCS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12
分子式C12H13N.CH4O3S
分子量267.34
溶解度≥ 13.4 mg/mL in DMSO, ≥ 46 mg/mL in EtOH with ultrasonic, ≥ 95.8 mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Rasagiline mesylate is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease. Target: Monoamine Oxidase (MAO)-BRasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug. Rasagiline is effective as monotherapy or adjunct to L-Dopa for patients with early and late Parkinson's disease (PD) [1]. Rasagiline inhibits MAO-B more potently than selegiline and has the advantage of once-daily dosing. In several large, randomized, placebo-controlled trials, rasagiline has demonstrated efficacy as monotherapy in early PD and as adjunctive therapy in advanced PD. In addition, rasagiline has been shown to have neuroprotective effects in in vitro and in vivo studies. The recently completed delayed-start ADAGIO (Attenuation of Disease Progression with Azilect Given Once-daily) trial suggests a potential disease-modifying effect for rasagiline 1 mg/day, though the clinical import of this finding has yet to be established [2]. Rasagiline has been found to be well tolerated and effective in the treatment of early PD and as adjunctive treatment in motor fluctuations. Whether rasagiline is associated with clinically significant neuroprotection (ie, disease modification) in PD is the subject of ongoing clinical trials [3].

References:
[1]. Weinreb, O., et al., Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol, 2010. 92(3): p. 330-44.
[2]. Lei D, et al. Synergistic neuroprotective effect of rasagiline and idebenone against retinal ischemia-reperfusion injury via the Lin28-let-7-Dicer pathway. Oncotarget. 2018 Jan 30;9(15):12137-12153.
[3]. Leegwater-Kim, J. and E. Bortan, The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging, 2010. 5: p. 149-56.
[4]. Chen, J.J., D.M. Swope, and K. Dashtipour, Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther, 2007. 29(9): p. 1825-49.