Pargyline 是一种不可逆的单胺氧化酶 (MAO) 抑制剂，对MAO-A和MAO-B的Ki分别为 13 μM 和 0.5 μM。Pargyline 具有降压和抗癌活性。
| 生物活性 | Pargyline is an irreversiblemonoamine oxidase(MAO)inhibitor withKis of 13 μM and 0.5 μM forMAO-AandMAO-B, respectively. Pargyline has antihypertensive and anticancer activities[1][2][3]. |
| IC50& Target[2] | MAO-B 0.5 μM (Ki) | MAO-A 13 μM (Ki) |
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体外研究
(In Vitro) | Pargyline (0.5-2 mM; 24-120 hours; LNCaP-LN3 cells) treatment inhibits the proliferation of prostate cancer cells in a time- and dose-dependent manner[2].
Pargyline (0.5-2 mM; 24-48 hours; LNCaP-LN3 cells) treatment decreases S phase and increases the G1 phase in the cells in a dose-dependent manner[2].
Pargyline (0.5 mM; 24 hours; LNCaP-LN3 cells) treatment increases the apoptotic cells[2].
Pargyline (2 mM; 48 hours; LNCaP-LN3 cells) treatment induces an increase of cytochrome c and a decrease of caspase-3 in the cells, but does not lead to a change of BCL-2 expression[2].
Cell Proliferation Assay[2] | Cell Line: | LNCaP-LN3 cells | | Concentration: | 0.5 mM, 1 mM, 1.5 mM or 2 mM | | Incubation Time: | 24 hours, 48 hours, 72 hours, 96 hours or 120 hours | | Result: | Inhibited the proliferation of prostate cancer cells in a time- and dose-dependent manner. |
Cell Cycle Analysis[2] | Cell Line: | LNCaP-LN3 cells | | Concentration: | 0.5 mM, 2 mM | | Incubation Time: | 24 hours, 48 hours | | Result: | The S phase ratio of the cells was decreased, while their G1 phase ratio was increased. |
Apoptosis Analysis[2] | Cell Line: | LNCaP-LN3 cells | | Concentration: | 0.5 mM | | Incubation Time: | 24 hours | | Result: | Increased the apoptotic cells. |
Western Blot Analysis[2] | Cell Line: | LNCaP-LN3 cells | | Concentration: | 2 mM | | Incubation Time: | 48 hours | | Result: | Induced an increase of cytochrome c and a decrease of caspase-3. |
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体内研究
(In Vivo) | Pargyline (10 mg/kg; iv) treatment induces a moderate (about 20 mm Hg) but persistent (48 h) decrease of systolic blood pressure in unanesthetized adult spontaneously hypertensive rats (SHR) but not in normotensive rats[3].
A low dose of Pargyline (200 μg; icv) injected directly into the brain lowered arterial pressure. The hypotensive action of Pargylline in SHR appears to be the consequence of Norepinephrine accumulating at an inhibitory α-adrenoceptor in brain[3].
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| 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: DMSO : 100 mg/mL(628.02 mM;Need ultrasonic) 配制储备液 | 1 mM | 6.2802 mL | 31.4011 mL | 62.8022 mL | | 5 mM | 1.2560 mL | 6.2802 mL | 12.5604 mL | | 10 mM | 0.6280 mL | 3.1401 mL | 6.2802 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (15.70 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (15.70 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 (15.70 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (15.70 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 (15.70 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (15.70 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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