Pargyline(Synonyms: 优降宁)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Pargyline (Synonyms: 优降宁) 纯度: 99.82%

Pargyline 是一种不可逆的单胺氧化酶 (MAO) 抑制剂,对 MAO-AMAO-BKi 分别为 13 μM 和 0.5 μM。Pargyline 具有降压和抗癌活性。

Pargyline(Synonyms: 优降宁)

Pargyline Chemical Structure

CAS No. : 555-57-7

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生物活性

Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-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)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

159.23

Formula

C11H13N

CAS 号

555-57-7

中文名称

优降宁;巴吉林;帕吉林

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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. C J Fowler, et al. The nature of the inhibition of rat liver monoamine oxidase types A and B by the acetylenic inhibitors clorgyline, l-deprenyl and pargyline. Biochem Pharmacol. 1982 Nov 15;31(22):3555-61.

    [2]. Hyung Tae Lee, et al. Effects of the monoamine oxidase inhibitors pargyline and tranylcypromine on cellular proliferation in human prostate cancer cells. Oncol Rep. 2013 Oct;30(4):1587-92.

    [3]. Fuentes JA, et al. Central mediation of the antihypertensive effect of pargyline in spontaneously hypertensive rats. Eur J Pharmacol. 1979 Jul 15;57(1):21-7.

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