Rasagiline Mesylate

立即咨询

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。

CAS NO:

161735-79-1

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

甲磺酸雷沙吉兰
(R)-AGN1135 mesylate
TVP1012 mesylate

产品介绍

Rasagiline (R-AGN1135) mesylate 是一种高效的不可逆的选择性线粒体单胺氧化酶 (MAO) 抑制剂，抑制大鼠脑 MAO B 和 MAO A 的IC₅₀分别为 4.43 nM 和 412 nM。

生物活性

Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversiblemitochondrialmonoamine oxidase(MAO) inhibitor withIC₅₀s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively^[1].

IC₅₀& Target^[1]

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^[2].

Cell Viability Assay^[2]

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^[3].

Animal Model:	(PLP)-α-synuclein transgenic mice over 6 months of age^[3]
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.

Clinical Trial

分子量

267.34

性状

Solid

Formula

C₁₃H₁₇NO₃S

CAS 号

161735-79-1

中文名称

雷沙吉兰甲磺酸；甲磺酸雷沙吉兰

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

In Vitro:

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.
请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (374.06 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。