| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Dopamine D2 and serotonin 5-HT1A receptors (partial agonist), serotonin 5-HT2A and 5-HT7 receptors (antagonist). Brilaroxazine's unique receptor profile is thought to contribute to its effects on vascular tone and inflammation. It also has affinity for other receptors, including alpha-1 adrenergic receptors.
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| ln Vitro |
Brilaroxazine exhibits partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors, and antagonist activity at serotonin 5-HT2A and 5-HT7 receptors. This receptor profile is distinct from that of other drugs used for PAH. In preclinical studies, it has been shown to reduce pulmonary arterial pressure and improve hemodynamic parameters.
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| ln Vivo |
Right ventricular (RV) hypertrophy, SO2, pulmonary hemodynamics, and alterations in pulmonary vascular structure are all markedly improved by braoxazine (oral gavage; 10 mg/kg; twice daily; 28 days) and its effects are limited in terms of both function and structure [1].
In vivo, brilaroxazine has demonstrated efficacy in animal models of pulmonary arterial hypertension. It has been shown to reduce pulmonary arterial pressure, improve cardiac output, and decrease vascular remodeling. These findings support its potential as a therapeutic agent for PAH. |
| Enzyme Assay |
In vitro receptor binding assays for brilaroxazine involve measuring its affinity for a panel of receptors, including D2, 5-HT1A, 5-HT2A, and 5-HT7, using radioligand binding techniques. Membranes from cells expressing the receptors are incubated with radiolabeled ligands and increasing concentrations of brilaroxazine. Ki values are determined from competition binding curves.
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| Cell Assay |
In vitro cellular assays for brilaroxazine involve treating cells expressing the target receptors with the compound and measuring its effects on receptor-mediated signaling, such as cAMP modulation or calcium mobilization. The compound's intrinsic activity is determined from these functional assays.
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| Animal Protocol |
Animal/Disease Models: SD-rat[2]
Doses: 10 mg/kg Route of Administration: po (oral gavage); twice a day; 28 days Experimental Results: Effective against PAH and alleviate the functional and structural effects of PAH caused by MCT. In vivo animal studies for brilaroxazine typically involve administration to rodent models of PAH, such as the monocrotaline-induced PAH model. Efficacy is assessed by measuring pulmonary arterial pressure, right ventricular hypertrophy, and vascular remodeling. The compound is typically administered orally. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for brilaroxazine is derived from clinical trials. The compound is well absorbed after oral administration. Its half-life and metabolic profile have been characterized. The compound is primarily metabolized in the liver.
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| Toxicity/Toxicokinetics |
Preclinical and clinical toxicity studies of brilaroxazine have been conducted. The compound is generally well tolerated. Common adverse effects may include headache, nausea, and dizziness. Comprehensive safety data is available from clinical trials.
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| References | |
| Additional Infomation |
Brilaroxazine (RP5063) is an investigational atypical antipsychotic drug developed by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder. Reviva Pharmaceuticals also plans to investigate RP5063 for the treatment of bipolar disorder, major depressive disorder, Alzheimer's disease-related psychosis/agitation, Parkinson's disease psychosis, attention deficit hyperactivity disorder (ADD/ADHD), and autism. As of May 2015, the drug was in a Phase III clinical trial for the treatment of schizophrenia.
Drug Indications Study for the treatment of schizophrenia and schizoaffective disorder. Brilaroxazine is an investigational drug being developed for the treatment of pulmonary arterial hypertension. It is a dopamine D2 and serotonin 5-HT1A receptor partial agonist, and an antagonist at serotonin 5-HT2A and 5-HT7 receptors. Its unique mechanism of action is thought to modulate neurotransmitter systems involved in vascular tone and inflammation. It has been evaluated in clinical trials for PAH. |
| Molecular Formula |
C22H25CL2N3O3
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|---|---|
| Molecular Weight |
450.36
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| Exact Mass |
449.127
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| CAS # |
1239729-06-6
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| PubChem CID |
46861612
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
643.0±55.0 °C at 760 mmHg
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| Flash Point |
342.7±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.593
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| LogP |
4.79
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
562
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PMKMNTBZJOXTJW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25Cl2N3O3/c23-17-4-3-5-19(22(17)24)27-11-9-26(10-12-27)8-1-2-13-29-16-6-7-20-18(14-16)25-21(28)15-30-20/h3-7,14H,1-2,8-13,15H2,(H,25,28)
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| Chemical Name |
6-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-4H-1,4-benzoxazin-3-one
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| Synonyms |
RP5063RP-5063
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~222.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2204 mL | 11.1022 mL | 22.2045 mL | |
| 5 mM | 0.4441 mL | 2.2204 mL | 4.4409 mL | |
| 10 mM | 0.2220 mL | 1.1102 mL | 2.2204 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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