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Brilaroxazine

🥰Excellent
Catalog No. T14782Cas No. 1239729-06-6
Alias RP5063

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.

Brilaroxazine
Other Forms of Brilaroxazine:
RP5063 HydrochlorideT247361708960-04-6
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Brilaroxazine

🥰Excellent
Purity: 99.36%
Catalog No. T14782Alias RP5063Cas No. 1239729-06-6
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$107In StockIn Stock
5 mg$263In StockIn Stock
10 mg$428In StockIn Stock
25 mg$737In StockIn Stock
50 mg$1,060In StockIn Stock
100 mg$1,450In StockIn Stock
200 mg$1,930In StockIn Stock
1 mL x 10 mM (in DMSO)$297In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.36%
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Product Introduction

Bioactivity
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-HT2A receptor:2.5 nM (Ki), 5-HT2B receptor:0.19 nM (Ki), 5-HT7 receptor:2.7 nM (Ki), 5-HT1A receptor:1.5 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].
SynonymsRP5063
Chemical Properties
Molecular Weight450.36
FormulaC22H25Cl2N3O3
Cas No.1239729-06-6
SmilesClc1cccc(N2CCN(CCCCOc3ccc4OCC(=O)Nc4c3)CC2)c1Cl
Relative Density.1.301 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2204 mL11.1022 mL22.2045 mL111.0223 mL
5 mM0.4441 mL2.2204 mL4.4409 mL22.2045 mL
10 mM0.2220 mL1.1102 mL2.2204 mL11.1022 mL
20 mM0.1110 mL0.5551 mL1.1102 mL5.5511 mL
50 mM0.0444 mL0.2220 mL0.4441 mL2.2204 mL
100 mM0.0222 mL0.1110 mL0.2220 mL1.1102 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
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Keywords

syndrome,ADHDSerotonin ReceptorRP-5063RP 5063PulmonaryParkinsonPAHInhibitorinhibithypertensionDopamineReceptorDopamine Receptordisorder,TourettedepressiveD4 receptorD4 ReceptorD3 ReceptorD3 receptorD2 receptorD2 ReceptorcardiacBrilaroxazineautismarterialAlzheimer5-hydroxytryptamine Receptor5HTReceptor5-HT7 Receptor5-HT75-HT2B Receptor5-HT2B5-HT2A Receptor5-HT2A5-HT1A Receptor5-HT1A5-HT Receptor5HT Receptor
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