PITOLISANT OXALATE
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $980 | Check With Us |
| 500mg | $1420 | Check With Us |
| 1g | $2130 | Check With Us |
: Cat #: V4309 CAS #: 362665-57-4 Purity ≥ 98%
Description: Pitolisant oxalate (formerly BF2649; BF2.649; Ciproxidine; Tiprolisant; Wakix), the oxalate salt of pitolisant, is a novel nonimidazole analog and an inverse agonist of the recombinant human histamine H3 receptor with Ki of 0.16 nM.
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| Molecular Weight (MW) | 385.88 |
|---|---|
| Molecular Formula | C₁₉H₂₈ClNO₅ |
| CAS No. | 362665-57-4 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| SMILES Code | ClC1=CC=C(CCCOCCCN2CCCCC2)C=C1.O=C(O)C(O)=O |
| Synonyms | FUB-649 oxalate, FUB649, BF-2649; FUB 649; BF2.649; BF2649 oxalate; B F2649; Pitolisant, Tiprolisant; Pitolisant oxalate; Pitolisant oxalate |
| 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 | 2.5915 mL | 12.9574 mL | 25.9148 mL | 51.8296 mL |
| 5mM | 0.5183 mL | 2.5915 mL | 5.1830 mL | 10.3659 mL |
| 10mM | 0.2591 mL | 1.2957 mL | 2.5915 mL | 5.1830 mL |
| 20mM | 0.1296 mL | 0.6479 mL | 1.2957 mL | 2.5915 mL |
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