Rasagiline mesylate (Synonyms:甲磺酸雷沙吉兰; (R-AGN1135 mesylate; TVP1012 mesylate))
目录号 : KM7567 CAS No. : 161735-79-1 纯度 : 98%

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。

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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.

体外研究

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

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

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.

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.
分子式
C12H13N.CH4O3S
分子量
267.34
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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