| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Brilaroxazine (RP-5063) is a potent anxiolytic drug for treating schizophrenia. It acts as a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs.
| 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].
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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. |
| References | |
| Additional Infomation |
Brilaroxazine (RP5063) is an investigational atypical antipsychotic which is under development by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder. Reviva Pharmaceuticals also intends to investigate RP5063 for the treatment of bipolar disorder, major depressive disorder, psychosis/agitation associated with Alzheimer's disease, Parkinson's disease psychosis, attention deficit hyperactivity disorder (ADD/ADHD), and autism. As of May 2015, it is in phase III clinical trials for schizophrenia.
Drug Indication Investigated for the treatment of schizophrenia and schizoaffective disorder. |
| Molecular Formula |
C22H25CL2N3O3
|
|---|---|
| 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
|
| Vapour Pressure |
0.0±1.9 mmHg at 25°C
|
| 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
|
| Heavy Atom Count |
30
|
| Complexity |
562
|
| Defined Atom Stereocenter Count |
0
|
| 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)
|
| Chemical Name |
6-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-4H-1,4-benzoxazin-3-one
|
| 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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