甲磺酸雷沙吉兰, 单胺氧化酶 B 抑制剂

MAO-B 选择性抑制剂
  • 10mM in DMSO
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
R409148-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 TVP-1012 | (1R)​-2,​3-​dihydro-​N-​2-​propyn-​1-​yl-1H-​inden-​1-​amine,methanesulfonate (1:1)
规格或纯度 10mM in DMSO
英文名称 Rasagiline Mesylate
生化机理 甲磺酸拉沙吉林(TVP-1012)是一种新型 MAO-B 抑制剂,用于治疗特发性帕金森病。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 单胺氧化酶 B 抑制剂
产品介绍

Rasagiline Mesylate是一种新型MAO-B抑制剂,用于治疗突发性帕金森病。A selective irreversible MAO-B inhibitor

Information

Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.
In vitro

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 vivo

Rasagiline 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.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

IC50 MAO-B, IC50: 4.43 nM

关联靶点(人)

MAOB Tclin 胺氧化酶[含黄素]B(Amine oxidase [flavin-containing] B) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MAOA Tclin 胺氧化酶[含黄素]A(Amine oxidase [flavin-containing] A) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES C[S](O)(=O)=O.C#CCNC1CCC2=CC=CC=C12
分子量 267.34

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 2 mg/mL (5.74 mM); Water: Insoluble; Ethanol: Insoluble;

安全和危险性(GHS)

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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