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Pitolisant

Name: Pitolisant
Brand: TargetMol
SKU: T60636
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T60636Cas No. 362665-56-3

Alias Tiprolisant, BF-2649, BF-2.649

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

Pitolisant

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Purity: 99.84%

Catalog No. T60636Alias Tiprolisant, BF-2649, BF-2.649Cas No. 362665-56-3

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

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$40	In Stock	In Stock
10 mg	$64	In Stock	In Stock
25 mg	$123	In Stock	In Stock
50 mg	$198	In Stock	In Stock
100 mg	$328	-	In Stock
500 mg	$787	-	In Stock
1 mL x 10 mM (in DMSO)	$44	-	In 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:99.84%

Appearance:Liquid

Color:Transparent

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	Pitolisant is a potent and selective nonimidazole inverse agonist that targets the recombinant human histamine H3 receptor, with a Ki of 0.16 nM.
Targets&IC50	H3 receptor:1.5 nM (EC50), H3 receptor:0.16 nM (Ki)
In vitro	When stimulating [35S]-thiophosphate-labeled GTPγS binding to recombinant human H3 receptors, Pitolisant (BF2.649) acts as a competitive antagonist with a Ki value of 0.16 nM. As a reverse agonist, its EC50 value is 1.5 nM, with intrinsic activity about 50% higher than that of ciproxifan[1].
In vivo	Pitolisant (BF2.649) dose-dependently enhances histamine levels in the mouse brain, with an ED50 value of 1.6 mg/kg p.o. This effect persists after repeated administration for 17 days[1].
Synonyms	Tiprolisant, BF-2649, BF-2.649

Chemical Properties

Molecular Weight	295.85
Formula	C₁₇H₂₆ClNO
Cas No.	362665-56-3
Smiles	Clc1ccc(CCCOCCCN2CCCCC2)cc1

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (270.41 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (11.15 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

	1mg	5mg	10mg	50mg
1 mM	3.3801 mL	16.9005 mL	33.8009 mL	169.0046 mL
5 mM	0.6760 mL	3.3801 mL	6.7602 mL	33.8009 mL
10 mM	0.3380 mL	1.6900 mL	3.3801 mL	16.9005 mL
20 mM	0.1690 mL	0.8450 mL	1.6900 mL	8.4502 mL
50 mM	0.0676 mL	0.3380 mL	0.6760 mL	3.3801 mL
100 mM	0.0338 mL	0.1690 mL	0.3380 mL	1.6900 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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