2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor Adrenergic Receptor
  4. Brexpiprazole

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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CAS No. : 913611-97-9

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ready for reconstitution
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Brexpiprazole:

Brexpiprazole Related Antibodies

Top Publications Citing Use of Products

    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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    α adrenergic receptor β adrenergic receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)[1][2].

    IC50 & Target

    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)

    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.

    Brexpiprazole Related Antibodies
    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.
    Molecular Weight

    433.57

    Formula

    C25H27N3O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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.

    • 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.

      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.
    • 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

    mg/kg

    Animal weight
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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.80%

    SDS (393 KB)

    COA (245 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    References

    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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    Brexpiprazole Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Brexpiprazole913611-97-9OPC-34712OPC34712OPC 347125-HT ReceptorDopamine ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorPC12orally activerecognition deficitsneurite outgrowthantipsychoticInhibitorinhibitorinhibit

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