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Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $107 | In Stock | In Stock | |
| 5 mg | $263 | In Stock | In Stock | |
| 10 mg | $428 | In Stock | In Stock | |
| 25 mg | $737 | In Stock | In Stock | |
| 50 mg | $1,060 | In Stock | In Stock | |
| 100 mg | $1,450 | In Stock | In Stock | |
| 200 mg | $1,930 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $297 | In Stock | In Stock |
| Description | Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases. |
| Targets&IC50 | 5-HT1A receptor:1.5 nM (Ki), 5-HT2B receptor:0.19 nM (Ki), 5-HT7 receptor:2.7 nM (Ki), 5-HT2A receptor:2.5 nM (Ki) |
| In vivo | Brilaroxazine (10 mg/kg) had efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH, with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes[3]. |
| Synonyms | RP5063 |
| Molecular Weight | 450.36 |
| Formula | C22H25Cl2N3O3 |
| Cas No. | 1239729-06-6 |
| Smiles | Clc1cccc(N2CCN(CCCCOc3ccc4OCC(=O)Nc4c3)CC2)c1Cl |
| Relative Density. | 1.301 g/cm3 (Predicted) |
| 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: 95 mg/mL (210.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.33 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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