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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 |
Description | Pitolisant (Tiprolisant) is a selective and potent non-imidazole recombinant human histamine H3 receptor antagonist for the study of excessive daytime sleepiness and sudden collapse in patients with episodic narcolepsy. |
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-2.649, BF-2649 |
Molecular Weight | 295.85 |
Formula | C17H26ClNO |
Cas No. | 362665-56-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (270.41 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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