PITOLISANT HCL
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $980 | Check With Us |
| 500mg | $1420 | Check With Us |
| 1g | $2130 | Check With Us |
: Cat #: V4308 CAS #: 903576-44-3 Purity ≥ 98%
Description: Pitolisant HCl (formerly also known as BF2.649; BF2649; Ciproxidine; Wakix) is a nonimidazole-based inverse agonist of the recombinant human histamine H3 receptor approved in 2019 for the treatment of excessive daytime sleepiness in adults with narcolepsy.
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| Molecular Weight (MW) | 332.309 |
|---|---|
| Molecular Formula | C17H27Cl2NO |
| CAS No. | 903576-44-3 |
| Storage | -20℃ for 3 years in powder formrrrr |
| -80℃ for 2 years in solvent | |
| SMILES Code | ClC1=CC=C(CCCOCCCN2CCCCC2)C=C1.[H]Cl |
| Synonyms | FUB-649, BF-2649; B F2649; FUB649, BF2649; FUB 649; BF2.649; Pitolisant, Tiprolisant; Pitolisant HCl; Pitolisant hydrochloride |
| Protocol | In Vitro | On the stimulation of guanosine 5′-O-(3-[35S]thio)triphosphate binding to this receptor, Pitolisant (BF2.649) 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. Pitolisant displaces [125I]iodoproxyfan binding from mouse brain cortical membranes with an IC50 value of 26.4±4.5 nM. Taking into account the Kd value of the radioligand (161±9 pM), the deduced Ki value for Pitolisant is 14±1 nM. Pitolisant displaces [125I]iodoproxyfan binding from membranes of rat glioma C6 cells stably expressing the human H3 receptor with an IC50 value of 4.2±0.2 nM. Taking into account the Kd value of the radioligand (50±4 pM), the deduced Ki value for Pitolisant is 2.7±0.5 nM. Pitolisant progressively reverses this response with a Hill coefficient close to unity and an IC50 value of 330±68 nM, leading to a Ki value of 17±4 nM. Pitolisant elicits a dose-dependent decrease of the basal-specific [35S]GTPγS binding to membranes with a maximal effect corresponding to 75±1% of the basal-specific binding and an EC50 value of 1.5±0.1 nM |
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These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.0092 mL | 15.0462 mL | 30.0925 mL | 60.1849 mL |
| 5mM | 0.6018 mL | 3.0092 mL | 6.0185 mL | 12.0370 mL |
| 10mM | 0.3009 mL | 1.5046 mL | 3.0092 mL | 6.0185 mL |
| 20mM | 0.1505 mL | 0.7523 mL | 1.5046 mL | 3.0092 mL |
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Method for preparing in vivo formulation:
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
Note:
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