1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Pargyline

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. Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Pargyline Chemical Structure

Pargyline Chemical Structure

CAS No. : 555-57-7

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Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
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10 mM * 1 mL in DMSO USD 66 In-stock
Liquid
500 mg USD 60 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

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]. Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[2]

MAO-B

0.5 μM (Ki)

MAO-A

13 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
BTI-TN-5B1-4 IC50
0.15 μM
Compound: Pargyline
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in production of H202 using p-tyramine as substrate incubated for 30 mins followed by substrate addition by horse radish peroxidase
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in production of H202 using p-tyramine as substrate incubated for 30 mins followed by substrate addition by horse radish peroxidase
[PMID: 31151057]
DU-145 GI50
218.89 μM
Compound: 3
Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 34908406]
PC-3 GI50
196.97 μM
Compound: 3
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 34908406]
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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

159.23

Formula

C11H13N

CAS No.
Appearance

Liquid (Density: 0.944 g/cm3)

Color

Colorless to light yellow

SMILES

C#CCN(C)CC1=CC=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (628.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (15.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (15.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.82%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 6.2802 mL 31.4011 mL 62.8022 mL 157.0056 mL
5 mM 1.2560 mL 6.2802 mL 12.5604 mL 31.4011 mL
10 mM 0.6280 mL 3.1401 mL 6.2802 mL 15.7006 mL
15 mM 0.4187 mL 2.0934 mL 4.1868 mL 10.4670 mL
20 mM 0.3140 mL 1.5701 mL 3.1401 mL 7.8503 mL
25 mM 0.2512 mL 1.2560 mL 2.5121 mL 6.2802 mL
30 mM 0.2093 mL 1.0467 mL 2.0934 mL 5.2335 mL
40 mM 0.1570 mL 0.7850 mL 1.5701 mL 3.9251 mL
50 mM 0.1256 mL 0.6280 mL 1.2560 mL 3.1401 mL
60 mM 0.1047 mL 0.5234 mL 1.0467 mL 2.6168 mL
80 mM 0.0785 mL 0.3925 mL 0.7850 mL 1.9626 mL
100 mM 0.0628 mL 0.3140 mL 0.6280 mL 1.5701 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Pargyline
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