Rasagiline (R-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。
| 生物活性 | Rasagiline (R-AGN1135) 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) |
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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 Proliferation 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. |
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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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(583.98 mM;Need ultrasonic) H2O : ≥ 5.88 mg/mL(34.34 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 5.8398 mL | 29.1988 mL | 58.3976 mL | | 5 mM | 1.1680 mL | 5.8398 mL | 11.6795 mL | | 10 mM | 0.5840 mL | 2.9199 mL | 5.8398 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。-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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (14.60 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.60 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (14.60 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.60 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (14.60 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.60 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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