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Pitolisant oxalate is a potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor, exhibiting a Ki of 0.16 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 1-2 weeks | 1-2 weeks | |
| 50 mg | $1,980 | 1-2 weeks | 1-2 weeks | |
| 100 mg | $2,500 | 1-2 weeks | 1-2 weeks |
| Description | Pitolisant oxalate is a potent and selective nonimidazole inverse agonist of the recombinant human histamine H3 receptor, exhibiting a Ki of 0.16 nM. |
| Targets&IC50 | H3 receptor:0.16 nM (Ki), H3 receptor:1.5 nM (EC50) |
| In vitro | Pitolisant 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. |
| In vivo | Administering Pitolisant at a single dose of 10 mg/kg 30 minutes before a 2 mg/kg b.w. dose of Olanzapine significantly affects immobility time in the FST. This drug sequence in mice significantly increases immobility duration compared to the control group in the FST and also decreases locomotor activity [3]. |
| Synonyms | Tiprolisant oxalate |
| Molecular Weight | 385.88 |
| Formula | C19H28ClNO5 |
| Cas No. | 362665-57-4 |
| Smiles | O=C(O)C(=O)O.ClC1=CC=C(C=C1)CCCOCCCN2CCCCC2 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (129.57 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (6.48 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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