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Loxapine succinate (Loxapac), a D2DR and D4DR inhibitor, is utilized in schizophrenia.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 50 mg | $33 | In Stock | In Stock | |
| 100 mg | $47 | In Stock | In Stock | |
| 200 mg | $76 | In Stock | In Stock | |
| 500 mg | $167 | Backorder | Backorder | |
| 1 mL x 10 mM (in DMSO) | $52 | In Stock | In Stock |
| Description | Loxapine succinate (Loxapac), a D2DR and D4DR inhibitor, is utilized in schizophrenia. |
| Targets&IC50 | 5-HT2 (bovine):6.6 nM(Ki), 5-HT2 (bovine):6.8 nM(Ki), 5-HT2 (human):6.2 nM(Ki), D4 receptor (human):7.5 nM(Ki), D2 receptor (human):24 nM(Ki) |
| In vitro | In rats, subcutaneous injection of Loxapine (0.3 mg/kg) induces general stiffness. In the rat brain, administering Loxapine (5 mg/kg) does not alter dopamine receptor density, but it reduces serotonin receptor density. |
| In vivo | Loxapine effectively facilitates the binding of [3H]ketanserin to 5-HT2 receptors in both the human frontal cortex (ki=6.2 nM) and the bovine frontal cortex (ki=6.6 nM). Additionally, in LPS-activated mixed glial cells, loxapine at concentrations of 0.2 μM, 2 μM, and 20 μM, successfully reduces the secretion of IL-1β and IL-2. |
| Synonyms | Loxapine succinate salt, Loxapac, Daxolin, Cloxazepin |
| Molecular Weight | 445.9 |
| Formula | C22H24ClN3O5 |
| Cas No. | 27833-64-3 |
| Smiles | OC(=O)CCC(=O)O.CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 2 mg/mL (4.49 mM), Sonication is recommended. DMSO: 82 mg/mL (183.9 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.4 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 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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