Brilaroxazine
Based on 1 Customer Validation
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
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- Pureté: 98.82%
- CAS No.: 1239729-06-6
- Formule: C22H25Cl2N3O3
- Masse moléculaire:450.36
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT1A Receptor 1.5 nM (Ki) |
5-HT1A Receptor |
5-HT2A Receptor |
5-HT2B Receptor |
5-HT7 Receptor |
5-HT2A Receptor 2.5 nM (Ki) |
5-HT2B Receptor 0.19 nM (Ki) |
5-HT7 Receptor 2.7 nM (Ki) |
D2 Receptor |
D3 Receptor |
D4 Receptor |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD-rats[2]
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Dosage:10 mg/kg
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Administration:Oral gavage; twice daily; 28 days
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Result:Had the efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1239729-06-6
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Appearance Solid
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Masse moléculaire 450.36
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Formule C22H25Cl2N3O3
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Color Off-white to light yellow
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SMILES
O=C1NC2=CC(OCCCCN3CCN(C(C=CC=C4Cl)=C4Cl)CC3)=CC=C2OC1
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Synonyms
RP5063
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : 100 mg/mL (222.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Reviva Pharmaceuticals Reports RP5063 Positive Efficacy Results for Memory Deficits
[2]. Bhat L, et al. Evaluation of the effects of RP5063, a novel, multimodal, serotonin receptor modulator, as single-agent therapy and co-administrated with sildenafil, bosentan, and treprostinil in a monocrotaline-induced pulmonary arterial hypertension rat model.Eur J Pharmacol. 2018 May 15;827:159-166. [Content Brief]
[3]. L. Bhat,et al. Rp5063 Prevents Monocrotaline Induced Pulmonary Arterial Hypertension In Rats.
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2204 mL | 11.1022 mL | 22.2045 mL | 55.5111 mL |
| 5 mM | 0.4441 mL | 2.2204 mL | 4.4409 mL | 11.1022 mL | |
| 10 mM | 0.2220 mL | 1.1102 mL | 2.2204 mL | 5.5511 mL | |
| 15 mM | 0.1480 mL | 0.7401 mL | 1.4803 mL | 3.7007 mL | |
| 20 mM | 0.1110 mL | 0.5551 mL | 1.1102 mL | 2.7756 mL | |
| 25 mM | 0.0888 mL | 0.4441 mL | 0.8882 mL | 2.2204 mL | |
| 30 mM | 0.0740 mL | 0.3701 mL | 0.7401 mL | 1.8504 mL | |
| 40 mM | 0.0555 mL | 0.2776 mL | 0.5551 mL | 1.3878 mL | |
| 50 mM | 0.0444 mL | 0.2220 mL | 0.4441 mL | 1.1102 mL | |
| 60 mM | 0.0370 mL | 0.1850 mL | 0.3701 mL | 0.9252 mL | |
| 80 mM | 0.0278 mL | 0.1388 mL | 0.2776 mL | 0.6939 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5551 mL |
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