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Pitolisant

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

Pitolisant

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 SizePriceAvailabilityQuantity
5 mg$40In Stock
10 mg$64In Stock
25 mg$123In Stock
50 mg$198In Stock
100 mg$328In Stock
500 mg$787In Stock
1 mL x 10 mM (in DMSO)$44In Stock
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Purity:99.84%
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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].
AliasTiprolisant, BF-2649, BF-2.649
Chemical Properties
Molecular Weight295.85
FormulaC17H26ClNO
Cas No.362665-56-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (270.41 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3801 mL16.9005 mL33.8009 mL169.0046 mL
5 mM0.6760 mL3.3801 mL6.7602 mL33.8009 mL
10 mM0.3380 mL1.6900 mL3.3801 mL16.9005 mL
20 mM0.1690 mL0.8450 mL1.6900 mL8.4502 mL
50 mM0.0676 mL0.3380 mL0.6760 mL3.3801 mL
100 mM0.0338 mL0.1690 mL0.3380 mL1.6900 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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