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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
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)267.34
FormulaC12H13N.CH4O3S
CAS No.161735-79-1 (mesylate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 53 mg/mL (198.2 mM)
Water: 53 mg/mL (198.2 mM)
Ethanol: 53 mg/mL (198.2 mM)
Solubility (In vivo)Saline: 30 mg/mL
SynonymsTVP101; TV 1030, TVP1022; Agn-1135; Azilect; TV-1030; HSDB 7699; Rasagiline; Racemic rasagiline; Agn 1135; Agn1135; rasagiline Mesylate; Rasagiline mesilate; Agilect; TVP-1022; TVP-101; N-2-propynyl-1-indanamine N-propargyl-1-aminoindan mesylate; rasagiline; rasagiline hydrochloride; TVP 101; TVP 1022; 1-Indanamine, N-2-propynyl-, (R)-; N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine methanesulfonate
实验参考方法
In Vitro

In vitro activity: Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro. Rasagiline prevents nuclear accumulation of GAPDH induced by N-methyl(R) salsolinol in SH-SY5Y cells. Rasagiline prevents the collapse in ΔΨm, and following apoptotic process, which indicates that mitochondria may determine the survival and death of the cells. Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and NGF withdrawal in partially neuronally differentiated PC12 cells and prevents the fall in mitochondrial membrane potential, the first step in cell death. Rasagiline is metabolized to its major metabolite aminoindan, selegiline gives rise to L-methamphetamine. Rasagiline directly activates PKC-MAP kinase pathway by a concentration and time dependent phosphorylation of p42 and p44 MAP kinase.

In VivoRasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. Rasagiline (0.2 mg/kg and 1 mg/kg) accelerates the recovery of motor function and spatial memory and reduces the cerebral oedema by about 40-50% in the mouse.
Animal modelMice
Formulation & Dosage0.2 mg/kg and 1 mg/kg
ReferencesBr J Pharmacol. 2001 Jan;132(2):500-6; Eur J Pharmacol. 1999 Feb 5;366(2-3):127-35.