Brexpiprazole
Based on 6 publication(s) in Google Scholar
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
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- Pureza: 99.80%
- No. CAS: 913611-97-9
- Fòrmula: C25H27N3O2S
- Peso molecular:433.57
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Brexpiprazole
More- Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
- Transl Psychiatry. 2025 Mar 8;15(1):77. [Abstract]
- Eur J Pharm Sci. 2025 Sep 27:214:107296. [Abstract]
- Eur J Pharmacol. 2021 Nov 15:911:174557. [Abstract]
- Pharmacol Rep. 2023 Apr;75(2):266-275. [Abstract]
- Fundam Clin Pharmacol. 2022 Dec;36(6):976-984. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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WB
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IHC
Ver todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
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5-HT1A Receptor 0.12 nM (Ki) |
5-HT1A Receptor |
5-HT2A Receptor |
5-HT2A Receptor 0.47 nM (Ki) |
D2L Receptor 0.3 nM (Ki) |
human noradrenergic α1B 0.17 nM (Ki) |
human noradrenergic α2C 0.59 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | CC50 |
50.57 μM
Compound: BREXPIPRAZOLE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
16.04 μM
Compound: BREXPIPRAZOLE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
| HEK293 | IC50 |
19.1 μg/mL
Compound: Brexpiprazole
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Cytotoxicity against human HEK293 cells assessed as reduction in cell viability
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability
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[PMID: 32122737] |
Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits[2]
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Dosage:0.01, 0.03 and 0.1 mg/kg
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Administration:Oral administration, once
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Result:Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.
Chemical Information
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No. CAS 913611-97-9
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Appearance Solid
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Peso molecular 433.57
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Fòrmula C25H27N3O2S
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Color White to off-white
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SMILES
O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1
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Synonyms
OPC-34712
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Brexpiprazole caused glycolipid metabolic disorder by inhibiting GLP1/GLP1R signaling in rats. [Abstract]2021 Aug;42(8):1267-1279. PMID: 33976388
Brexpiprazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
To evaluate the effect of the new APD Brexpiprazole (Bre) on glycolipid metabolism during 28 days, rats were randomly divided into four groups, with six female and six male rats in each group: (1) the vehicle group, rats received a blank sweet cookie dough pellet; (2) the Ola group, rats were treated with Ola (1.0 mg/kg); (3) the Ari group, rats were treated with Ari (1.0 mg/kg); (4) the Bre group, rats were treated with Bre (0.5 mg/kg).
Brexpiprazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
The rats treated with Ola, Ari, or Brexpiprazole (Bre, 0.5 mg/kg) had different degrees of weight gain.
Brexpiprazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
The rats' FBG was elevated obviously after 3 weeks administration of Ola or Brexpiprazole (Bre, 0.5 mg/kg), while the significant increase of FBG in Ari group only appeared at the 4th week.
Brexpiprazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
Both the GLP1 expressions in pancreas and small intestine were restrained by Ola or Brexpiprazole (Bre) and a similar effect was observed in GLP1 gene proglucagon (Gcg) by qPCR analysis.
Brexpiprazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
The pancreas H&E staining exhibited clear and well-organized structure of islets in the vehicle and Ari group rats, but abnormal histological changes such as vacuolization and islet size reduction were detected in both Ola and Brexpiprazole (Bre) groups.
Brexpiprazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Aug;42(8):1267-1279. [Abstract]
From the liver H&E staining, we could clearly see the vacuolization in Bre treated rats.
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Transl Psychiatry
Fine-tuning of dopamine receptor signaling with aripiprazole counteracts ketamine's dissociative action, but not its antidepressant effect. [Abstract]2025 Mar 8;15(1):77. PMID: 40057507 -
Eur J Pharm Sci
Repurposing of FDA-approved drugs by targeting SIRT2 to alleviate inflammatory response and kidney injury. [Abstract]2025 Sep 27:214:107296. PMID: 41022315 -
Eur J Pharmacol
2021 Nov 15:911:174557. PMID: 34626593 -
Pharmacol Rep
Agonistic properties of a series of psychotropic drugs at 5-HT1A receptors in rat and human brain membranes determined by [35S]GTPγS binding assay. [Abstract]2023 Apr;75(2):266-275. PMID: 36637685 -
Fundam Clin Pharmacol
Receptor density influences the recruitment bias of aripiprazole and brexpiprazole at the dopamine D2L receptor. [Abstract]2022 Dec;36(6):976-984. PMID: 35767599
Solvente y solubilidad
DMSO : 25 mg/mL (57.66 mM; ultrasonic and warming and heat to 80°C; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.77 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3064 mL | 11.5322 mL | 23.0643 mL | 57.6608 mL |
| 5 mM | 0.4613 mL | 2.3064 mL | 4.6129 mL | 11.5322 mL | |
| 10 mM | 0.2306 mL | 1.1532 mL | 2.3064 mL | 5.7661 mL | |
| 15 mM | 0.1538 mL | 0.7688 mL | 1.5376 mL | 3.8441 mL | |
| 20 mM | 0.1153 mL | 0.5766 mL | 1.1532 mL | 2.8830 mL | |
| 25 mM | 0.0923 mL | 0.4613 mL | 0.9226 mL | 2.3064 mL | |
| 30 mM | 0.0769 mL | 0.3844 mL | 0.7688 mL | 1.9220 mL | |
| 40 mM | 0.0577 mL | 0.2883 mL | 0.5766 mL | 1.4415 mL | |
| 50 mM | 0.0461 mL | 0.2306 mL | 0.4613 mL | 1.1532 mL |
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