Art. -Nr.: HY-15780

Brexpiprazole

(Synonyms: OPC-34712)

6 Cited Publications

Kundenbewertung

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 D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

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Reinheit: 99.80%
CAS. Nr.: 913611-97-9
Formel: C₂₅H₂₇N₃O₂S
Molecular Weight:433.57

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Brexpiprazole Chemical Structure

CAS. Nr.: 913611-97-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

5-HT_1A Receptor

0.12 nM (Ki)

5-HT_1A Receptor

5-HT_2A Receptor

0.47 nM (Ki)

D_2L Receptor

0.3 nM (Ki)

human noradrenergic α_1B

0.17 nM (Ki)

human noradrenergic α_2C

0.59 nM (Ki)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	50.57 μM Compound: BREXPIPRAZOLE	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	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	16.04 μM Compound: BREXPIPRAZOLE	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	10.21203/rs.3.rs-23951/v1
HEK293	IC₅₀	19.1 μg/mL Compound: Brexpiprazole	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability Cytotoxicity against human HEK293 cells assessed as reduction in cell viability	[PMID: 32122737]

In Vitro

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.

In Vivo

Brexpiprazole (0-0.1 mg/kg; p.o.; once) improves social recognition deficits in mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits^[2]
Dosage:

0.01, 0.03 and 0.1 mg/kg
Administration:

Oral administration, once
Result:

Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.

Chemical Information

CAS. Nr. 913611-97-9
Appearance Solid
Molecular Weight 433.57
Formel C₂₅H₂₇N₃O₂S
Color White to off-white
SMILES

O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1
Synonyms

OPC-34712
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All In Vivo Efficacy StudyWBIHC

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Journal Impact Factor

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.
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

Receptor density influences ligand-induced dopamine D2L receptor homodimerization. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Brexpiprazole

6 Cited Publications

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Brexpiprazole

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Publications Citing Use of MedChemExpress (MCE) Brexpiprazole

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Brexpiprazole Related Classifications

Art. -Nr.: HY-15780