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Pitolisant oxalate

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Catalog No. T12491Cas No. 362665-57-4
Alias Tiprolisant oxalate

Pitolisant oxalate is a potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor, exhibiting a Ki of 0.16 nM.

Pitolisant oxalate

Pitolisant oxalate

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Catalog No. T12491Alias Tiprolisant oxalateCas No. 362665-57-4
Pitolisant oxalate is a potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor, exhibiting a Ki of 0.16 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,5201-2 weeks1-2 weeks
50 mg$1,9801-2 weeks1-2 weeks
100 mg$2,5001-2 weeks1-2 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Pitolisant oxalate is a potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor, exhibiting a Ki of 0.16 nM.
Targets&IC50
H3 receptor:0.16 nM (Ki), H3 receptor:1.5 nM (EC50)
In vitro
Pitolisant behaves as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity ~50% higher than that of ciproxifan.
In vivo
Administering Pitolisant at a single dose of 10 mg/kg 30 minutes before a 2 mg/kg b.w. dose of Olanzapine significantly affects immobility time in the FST. This drug sequence in mice significantly increases immobility duration compared to the control group in the FST and also decreases locomotor activity [3].
SynonymsTiprolisant oxalate
Chemical Properties
Molecular Weight385.88
FormulaC19H28ClNO5
Cas No.362665-57-4
SmilesO=C(O)C(=O)O.ClC1=CC=C(C=C1)CCCOCCCN2CCCCC2
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: 50 mg/mL (129.57 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (6.48 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 mM2.5915 mL12.9574 mL25.9148 mL129.5740 mL
5 mM0.5183 mL2.5915 mL5.1830 mL25.9148 mL
10 mM0.2591 mL1.2957 mL2.5915 mL12.9574 mL
20 mM0.1296 mL0.6479 mL1.2957 mL6.4787 mL
50 mM0.0518 mL0.2591 mL0.5183 mL2.5915 mL
100 mM0.0259 mL0.1296 mL0.2591 mL1.2957 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

You can also refer to dose conversion for different animals. More Dose Conversion

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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