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Pergolide mesylate

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Catalog No. T2226Cas No. 66104-23-2
Alias Pergolide methanesulfonate, Pergolide mesylate salt, LY127809

Pergolide mesylate salt(LY127809) is a long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.

Pergolide mesylate

Pergolide mesylate

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🥰Excellent
Purity: 99.70%
Catalog No. T2226Alias Pergolide methanesulfonate, Pergolide mesylate salt, LY127809Cas No. 66104-23-2
Pergolide mesylate salt(LY127809) is a long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$47In StockIn Stock
10 mg$67In StockIn Stock
25 mg$117In StockIn Stock
50 mg$187In StockIn Stock
1 mL x 10 mM (in DMSO)$52In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.70%
Appearance:Solid
Color:White
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Product Introduction

Pergolide mesylate AI Summary
Pergolide mesylate exhibits a wide range of bioactivities across various biological systems and organisms. It shows high in vitro binding affinity towards dopamine receptors in rat and bovine membranes and induces behavioral and biochemical effects in rats, such as rotations, decreased dopamine turnover, stereotypies, and inhibition of prolactin release. Additionally, it induces emesis in Beagle dogs and has a lethal dose (LD50) in male mice via intraperitoneal administration. Notably, it also inhibits plasma prolactin levels in male Sprague-Dawley rats for over 22 hours post-oral administration. In terms of antiplasmodial activity, Pergolide mesylate demonstrates varying IC50 values against different strains of Plasmodium falciparum, ranging from 3981.07 nM to 12589.25 nM, indicating potential as an anti-malarial agent. It also shows inhibitory effects against the proliferation of various Plasmodium falciparum lines with potencies from 4466.8 nM to 12589.3 nM. The compound has additional bioactivities, such as inhibiting sodium fluorescein uptake in OATP1B3 and OATP1B1 transfected CHO cells by over 85% at 10 µM and inhibiting transport activities of human BSEP, MRP2, MRP3, and MRP4 in membrane vesicle assays with IC50 values greater than 133,000 nM. Regarding antiviral properties, Pergolide mesylate shows modest activity against SARS-CoV-2 in various cellular models. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and Vero E6 cells, though with relatively low inhibition indices. It also shows negligible inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM. Additionally, Pergolide mesylate demonstrates minor antibacterial and antifungal activities, inhibiting the growth of several bacterial strains such as Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus, with varying degrees of efficacy. However, it exhibits minimal to negative activity against Candida albicans and Cryptococcus neoformans..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Pergolide mesylate salt(LY127809) is a long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.
SynonymsPergolide methanesulfonate, Pergolide mesylate salt, LY127809
Chemical Properties
Molecular Weight410.59
FormulaC20H30N2O3S2
Cas No.66104-23-2
SmilesCS(O)(=O)=O.CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3cccc2c13
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (133.95 mM), Sonication is recommended.
H2O: 40 mg/mL (97.42 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.87 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.4355 mL12.1776 mL24.3552 mL121.7760 mL
5 mM0.4871 mL2.4355 mL4.8710 mL24.3552 mL
10 mM0.2436 mL1.2178 mL2.4355 mL12.1776 mL
20 mM0.1218 mL0.6089 mL1.2178 mL6.0888 mL
50 mM0.0487 mL0.2436 mL0.4871 mL2.4355 mL
DMSO
1mg5mg10mg50mg
100 mM0.0244 mL0.1218 mL0.2436 mL1.2178 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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