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Pargyline hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pargyline hydrochloride图片
CAS NO:306-07-0

优降宁盐酸盐;盐酸帕吉林;巴吉林盐酸盐
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。
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)

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.
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].

分子量

195.69

性状

Solid

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 mg5 mg10 mg
1 mM5.1101 mL25.5506 mL51.1012 mL
5 mM1.0220 mL5.1101 mL10.2202 mL
10 mM0.5110 mL2.5551 mL5.1101 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。

    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
  • 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。

    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
  • 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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