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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
🥰Excellent
Purity: 98.00%
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $107 | In Stock | |
| 5 mg | $263 | In Stock | |
| 10 mg | $428 | In Stock | |
| 25 mg | $737 | In Stock | |
| 50 mg | $1,060 | In Stock | |
| 100 mg | $1,450 | In Stock | |
| 500 mg | $2,880 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $387 | In Stock |
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Purity:98.00%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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-HT2B receptor:0.19 nM (Ki), 5-HT2A receptor:2.5 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]. |
| Alias | 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 95 mg/mL (210.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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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:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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 DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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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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