Pargyline hydrochloride(Synonyms: 优降宁盐酸盐;盐酸帕吉林;巴吉林盐酸盐)

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Pargyline hydrochloride (Synonyms: 优降宁盐酸盐;盐酸帕吉林;巴吉林盐酸盐) 纯度: 99.91%

Pargyline hydrochloride 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 hydrochloride 具有降压和抗癌活性。

Pargyline hydrochloride(Synonyms: 优降宁盐酸盐;盐酸帕吉林;巴吉林盐酸盐)

Pargyline hydrochloride Chemical Structure

CAS No. : 306-07-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
500 mg ¥500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

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生物活性

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

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

195.69

Formula

C11H14ClN

CAS 号

306-07-0

中文名称

优降宁盐酸盐;盐酸帕吉林;巴吉林盐酸盐

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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°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 (12.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.78 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 (12.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.78 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 (12.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.78 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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