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Mepyramine maleate

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Catalog No. T1232Cas No. 59-33-6
Alias Pyrilamine maleate

Mepyramine maleate (Pyrilamine maleate) is a histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.

Mepyramine maleate

Mepyramine maleate

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Purity: 99.92%
Catalog No. T1232Alias Pyrilamine maleateCas No. 59-33-6
Mepyramine maleate (Pyrilamine maleate) is a histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
500 mg$55In StockIn Stock
1 g$78-In Stock
1 mL x 10 mM (in DMSO)$29In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.92%
Appearance:Solid
Color:White
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Product Introduction

Mepyramine maleate AI Summary
Mepyramine maleate demonstrates in vitro anticholinergic activity with a Kd of 3981.07 nM and in vitro antihistaminic activity with a Kd of 0.4169 nM. It exhibits significant antiplasmodial activity against various strains of Plasmodium falciparum, with IC50 values of 12589.25 nM (Dd2), 7943.28 nM (GB4), and 5011.87 nM (W2) after 72 hours determined via SYBR green assay. Additionally, Mepyramine maleate shows broad bioactivity including, but not limited to, inhibition of several key enzymes and receptors, modulation of gene expression, and antiviral effects. Specific bioassays indicate it can inhibit human tyrosyl-DNA phosphodiesterase 1 (TDP1), AmpC Beta-Lactamase, Bloom's syndrome helicase (BLM), Histone Lysine Methyltransferase G9a, and others. It reduces sodium fluorescein uptake in OATP1B3-transfected CHO cells by 101.36% and in OATP1B1-transfected CHO cells by 68.75% at 10 µM concentration. Despite low inhibition of cell viability in SARS-CoV-2-infected Vero E6 cells (inhibition index = 0.1616), it shows 46.34% inhibition of SARS-CoV-2-induced cytotoxicity in Caco-2 cells at 10 µM after 48 hours. Furthermore, it inhibits the SARS-CoV-2 3CL-Pro protease by 22.97% at 20 µM..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Mepyramine maleate (Pyrilamine maleate) is a histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
SynonymsPyrilamine maleate
Chemical Properties
Molecular Weight401.47
FormulaC21H27N3O5
Cas No.59-33-6
SmilesN(c1ccccn1)(Cc1ccc(cc1)OC)CCN(C)C.C(=C\C(=O)O)\C(=O)O
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (112.09 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.98 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
DMSO
1mg5mg10mg50mg
1 mM2.4908 mL12.4542 mL24.9085 mL124.5423 mL
5 mM0.4982 mL2.4908 mL4.9817 mL24.9085 mL
10 mM0.2491 mL1.2454 mL2.4908 mL12.4542 mL
20 mM0.1245 mL0.6227 mL1.2454 mL6.2271 mL
50 mM0.0498 mL0.2491 mL0.4982 mL2.4908 mL
100 mM0.0249 mL0.1245 mL0.2491 mL1.2454 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:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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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