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Pitolisant
🥰Excellent
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
🥰Excellent
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 | Availability | Quantity |
|---|---|---|---|
| 5 mg | $40 | In Stock | |
| 10 mg | $64 | In Stock | |
| 25 mg | $123 | In Stock | |
| 50 mg | $198 | 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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Purity:99.84%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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:0.16 nM (Ki), H3 receptor:1.5 nM (EC50) |
| 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]. |
| Alias | Tiprolisant, BF-2649, BF-2.649 |
| Molecular Weight | 295.85 |
| Formula | C17H26ClNO |
| Cas No. | 362665-56-3 |
| Smiles | Clc1ccc(CCCOCCCN2CCCCC2)cc1 |
Storage & Solubility Information
| Storage | Powder: -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 | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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