Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rasagiline Mesylate (AGN1135) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 253 | 现货 | ||
50 mg | ¥ 418 | 现货 | ||
100 mg | ¥ 671 | 现货 | ||
500 mg | ¥ 1,675 | 现货 |
产品描述 | Rasagiline Mesylate (AGN1135) is a novel MAO-B inhibitor, which can treat idiopathic Parkinson's disease. |
靶点活性 | MAO-A:412 nM, MAO-B:4.43 nM |
体外活性 | 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. [1] 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. [2] 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. [3] 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. [4] |
体内活性 | Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. [1] 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. [5] |
别名 | TVP1012, 甲磺酸雷沙吉兰, AGN1135, Azilect |
分子量 | 267.34 |
分子式 | C13H17NO3S |
CAS No. | 161735-79-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 93.51mM
DMSO: 198.2 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 3.7406 mL | 18.7028 mL | 37.4056 mL | 93.5139 mL |
5 mM | 0.7481 mL | 3.7406 mL | 7.4811 mL | 18.7028 mL | |
10 mM | 0.3741 mL | 1.8703 mL | 3.7406 mL | 9.3514 mL | |
20 mM | 0.187 mL | 0.9351 mL | 1.8703 mL | 4.6757 mL | |
50 mM | 0.0748 mL | 0.3741 mL | 0.7481 mL | 1.8703 mL | |
DMSO | 100 mM | 0.0374 mL | 0.187 mL | 0.3741 mL | 0.9351 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rasagiline Mesylate 161735-79-1 Apoptosis Autophagy Metabolism Neuroscience MAO Monoamine Oxidase Rasagiline inhibit TVP1012 甲磺酸雷沙吉兰 AGN 1135 AGN-1135 Inhibitor AGN1135 (R)-AGN1135 Azilect TVP 1012 TVP-1012 inhibitor