PITOLISANT
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 | To Be Confirmed |
| 500mg | $1500 | To Be Confirmed |
| 1g | $2250 | To Be Confirmed |
: Cat #: V4307 CAS #: 362665-56-3 Purity ≥ 98%
Description: Pitolisant (formerly BF2.649; Tiprolisant; BF2649; Ciproxidine; Wakix) is a novel, potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor with Ki of 0.16 nM.
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- Related Biological Data
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| Molecular Weight (MW) | 295.85 |
|---|---|
| Molecular Formula | C17H26ClNO |
| CAS No. | 362665-56-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent |
| 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 |
|---|
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 | 3.3801 mL | 16.9005 mL | 33.8009 mL | 67.6018 mL |
| 5mM | 0.6760 mL | 3.3801 mL | 6.7602 mL | 13.5204 mL |
| 10mM | 0.3380 mL | 1.6900 mL | 3.3801 mL | 6.7602 mL |
| 20mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 3.3801 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
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PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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