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Rasagiline Mesylate

MAO-B抑制剂,Rasagiline甲磺酸盐是MAO-B抑制剂，可作用于原发性帕金森病

目录号: PC12516 纯度: ≥98%

CAS No. :161735-79-1

商品编号	规格	价格	会员价	是否有货	数量
PC12516-50mg	50mg	¥490.00	请登录
PC12516-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称	Rasagiline Mesylate
中文别名	甲磺酸雷沙吉兰;(R)-N-2-丙炔基-1-氢化茚胺甲磺酸盐;甲磺酸雷沙吉兰 ;Rasagiline Mesylate;甲磺酸雷沙吉兰标准品;雷沙吉兰甲磺酸盐;(R)-N-(2-丙炔-1-基)-1-氨基茚满甲磺酸盐;(R)-N-炔丙基-1-氨基茚满甲磺酸盐;磺酸雷沙吉兰;雷沙吉兰甲磺酸;马来酸雷沙吉兰;雷沙吉兰葡萄糖醛酸苷;甲磺酸雷沙吉兰(R)-N-2-丙炔基-1-氢化茚胺甲磺酸盐
英文名称	Rasagiline Mesylate
英文别名	(R)-N-(Prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine methanesulfonate;Rasagiline mesylate;1H-Inden-1-amine, 2,3-dihydro-N-2-propyn-1-yl-, (1R)-, methanesulfonate (1:1);AGN1135;methanesulfonic acid,(1R)-N-prop-2-ynyl-2,3-dihydro-1H-inden-1-amine;TVP1012;(1R)-2,3-Dihydro-N-2-propynl-1H-inden-1-amine methanesulfonate;N-Propargyl-1(R)-aminoindan methanesulfonate;TVP-1012;(R)-N-Propargyl-1-indanamine Methanesulfonate;(R)-N-(2-Propyn-1-yl)-1-indanamine Methanesulfonate;(R)-N-2-Propynyl-1-indanamine methanesulfonate;Azilect;Agilect;TVP-101;TV 1012;Unii-lh8C2ji290;Rasagiline nesylate;RASAGILINE MESILATE;RASAGILINE GLUCURONIDE
Cas No.	161735-79-1
分子式	C₁₂H₁₃N^.CH₄O₃S
分子量	267.34
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively.

性状

Solid

IC50 & Target[1][2]

rMAO-B

4.43 nM (IC₅₀)

rMAO-A

412 nM (IC₅₀)

体外研究(In Vitro)

Rasagiline (0.25 nM; 96 hours) significantly increases the proliferation rates of SH-SY5Y and 1242-MG upon Dexamethasone (10 μM) treatment.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Neuroblastoma SH-SY5Y, and glioblastoma 1242-MG
Concentration:	0.25 nM
Incubation Time:	96 hours
Result:	Caused ~60% increase in the cell proliferation rate for SH-SY5Y cells treated with Dexamethasone. Caused ~35% increase in cell proliferation rate for 1242-MG cells treated with Dexamethasone.

体内研究(In Vivo)

Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Motor behavioural tests show improvements in motor deficits associated with 2.5 mg/kg Rasagiline therapy.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	(PLP)-α-synuclein transgenic mice over 6 months of age
Dosage:	Low-(0.8 mg/kg b.w.) and high dose (2.5 mg/kg b. w.)
Administration:	Administered subcutaneously every 24 h for a total period of 4 weeks (from day 1 till day 28 of the experiment).
Result:	Low dose treatment did not show protective efficacy in striatum with number of neurons similar to placebo treated MSA mice. High dose was associated with about 15% rescue of DARPP-32 immunoreactive striatal neurons. Low dose treatment had no effect on nigral neuronal loss, but high dose completely protected nigral neurons with numbers comparable to healthy controls.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. M B Youdim, et al. Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6. [Information]

[2]. Shawna Tazik, et al. Comparative neuroprotective effects of Rasagiline and aminoindan with selegiline on dexamethasone-induced brain cell apoptosis. Neurotox Res. 2009 Apr;15(3):284-90. [Information]

[3]. Nadia Stefanova, et al. Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Exp Neurol. 2008 Apr;210(2):421-7. [Information]

溶解度数据

体外研究:

H₂O : 25 mg/mL (93.51 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7406 mL	18.7028 mL	37.4056 mL
5 mM	0.7481 mL	3.7406 mL	7.4811 mL
10 mM	0.3741 mL	1.8703 mL	3.7406 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (374.06 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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