Pargyline hydrochloride 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 hydrochloride 具有降压和抗癌活性。
生物活性 | Pargyline hydrochloride is an irreversiblemonoamine oxidase(MAO)inhibitor withKis of 13 μM and 0.5 μM forMAO-AandMAO-B, respectively. Pargyline hydrochloride 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: H2O : 100 mg/mL(511.01 mM;Need ultrasonic) DMSO : ≥ 32 mg/mL(163.52 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 5.1101 mL | 25.5506 mL | 51.1012 mL | 5 mM | 1.0220 mL | 5.1101 mL | 10.2202 mL | 10 mM | 0.5110 mL | 2.5551 mL | 5.1101 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: 25 mg/mL (127.75 mM); Clear solution; Need ultrasonic and warming 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (10.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.63 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (10.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.63 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (10.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.63 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 20.8 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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