| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Brexpiprazole (formerly OPC-34712; OPC34712; Rexulti) is a novel D2 dopamine partial agonist [also called serotonin-dopamine activity modulator (SDAM)] approved as an atypical antipsychotic drug. IT inhibits 5-HT2A receptor with a Ki value of 0.47 nMr. Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD). Brexpiprazole was approved on 7/10/2015 for the treatment of schizophrenia, and as an adjunctive treatment for depression.
| ln Vitro |
In PC12 cells, breexpipromaze (0-1.0 μM, 4 days) dose-dependently promotes NGF-induced neurite outgrowth [1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6NCrSlc mice, dizozepine (0.1 mg/kg)-induced social cognitive deficits [2]. 0.01, 0.03 and 0.1 mg/kg.
Route of Administration: Take once orally. Experimental Results: Significant improvement of social cognitive deficits caused by dizocycline without sedation or reduction in exploratory behavior. |
| References |
[1]. Ishima T, et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin-dopamine activity modulator: a role for serotonin 5-HT1A and 5-HT2A receptors. Eur Neuropsychopharmacol. 2015 Apr;25(4):505-11.
[2]. Yoshimi N, et al. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. Eur Neuropsychopharmacol. 2015 Mar;25(3):356-64. |
| Molecular Formula |
C25H27N3O2S
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|---|---|
| Molecular Weight |
433.5658
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| CAS # |
913611-97-9
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| Related CAS # |
Brexpiprazole-d8-1;1427049-19-1;Brexpiprazole hydrochloride;913612-38-1;Brexpiprazole-d8;1427049-21-5
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| SMILES |
S1C([H])=C([H])C2C1=C([H])C([H])=C([H])C=2N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])C([H])([H])OC2C([H])=C([H])C3C([H])=C([H])C(N([H])C=3C=2[H])=O)C([H])([H])C1([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~25 mg/mL (~57.66 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.77 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.77 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 | 2.3064 mL | 11.5322 mL | 23.0643 mL | |
| 5 mM | 0.4613 mL | 2.3064 mL | 4.6129 mL | |
| 10 mM | 0.2306 mL | 1.1532 mL | 2.3064 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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