Cat. No.: HY-14546

Aripiprazole

(Synonyms: OPC-14597)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

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Pureté: 99.95%
CAS No.: 129722-12-9
Formule: C₂₃H₂₇Cl₂N₃O₂
Masse moléculaire:448.39

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Aripiprazole Chemical Structure

CAS No.: 129722-12-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target

5-HT_1A Receptor

4.2 nM (Ki)

5-HT_1A Receptor

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

D₂ Receptor

D₃ Receptor

D₄ Receptor

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

Voir tous les produits spécifiques à Isoform Dopamine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	7.6 nM Compound: 1a	Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay	[PMID: 23237836]
HEK293	EC₅₀	>5 μM Compound: Aripiprazole	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	>5 μM Compound: Aripiprazole	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	>5 μM Compound: Aripiprazole	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	>5 μM Compound: Aripiprazole	Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	160 nM Compound: 2a, Aripiprazole	Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay	[PMID: 24831693]
HEK293	EC₅₀	20 nM Compound: 2a, Aripiprazole	Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay	[PMID: 24831693]
HEK293	IC₅₀	>100 μM Compound: 1	Cytotoxicity against HEK293 cells measured after 24 hrs by MTT assay Cytotoxicity against HEK293 cells measured after 24 hrs by MTT assay	[PMID: 35176563]
HEK293	IC₅₀	>500 μM Compound: aripiprazole	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	11 nM Compound: 2a, Aripiprazole	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	[PMID: 24831693]
HEK293	IC₅₀	130 μM Compound: aripiprazole	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	239 μM Compound: aripiprazole	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK-293T	EC₅₀	1 nM Compound: 1	Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay	[PMID: 22845053]
HEK-293T	EC₅₀	1100 nM Compound: Aripiprazole	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	[PMID: 28489379]
HEK-293T	EC₅₀	130 nM Compound: Aripiprazole	Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding	[PMID: 28489379]
HEK-293T	EC₅₀	160 nM Compound: 1a	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	[PMID: 28248104]
HEK-293T	EC₅₀	20 nM Compound: 1a	Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	[PMID: 28248104]
HEK-293T	EC₅₀	39 nM Compound: 1a	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	[PMID: 28248104]
HEK-293T	EC₅₀	740 nM Compound: Aripiprazole	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	[PMID: 28489379]

In Vitro

Aripiprazole potently activates D2 receptor-mediated inhibition of cAMP accumulation^[1].
Aripiprazole shows a greater anti-inflammatory effect on TNF-α, IL-13, IL-17α and fractalkine^[3].

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

In Vivo

Aripiprazole (0-3 mg/kg, IP, daily) shows some anxiolytic properties^[4].

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

Animal Model:

WAG/Rij rats (N = 6 per dose, 6 months, administration of a mixture of tiletamine/zolazepam)^[4]
Dosage:

0, 0.3, 1, 3 mg/kg
Administration:

IP, 1 mL/kg, every day at 5 p.m. until the end of the experiments
Result:

Showed some anxiolytic properties with the 1 mg/kg dose being the most active.

Chemical Information

CAS No. 129722-12-9
Appearance Solid
Masse moléculaire 448.39
Formule C₂₃H₂₇Cl₂N₃O₂
Color White to off-white
SMILES

O=C1NC2=C(C=CC(OCCCCN3CCN(C4=CC=CC(Cl)=C4Cl)CC3)=C2)CC1
Synonyms

OPC-14597
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (11)

All In Vivo Efficacy Study

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Journal Impact Factor

Nat Neurosci

Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. [Abstract]

2022 Jan;25(1):39-49. PMID: 34887590
Acta Pharmacol Sin

Brexpiprazole caused glycolipid metabolic disorder by inhibiting GLP1/GLP1R signaling in rats. [Abstract]

2021 Aug;42(8):1267-1279. PMID: 33976388
Chemosphere

Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]

2019 Jun:225:378-387. PMID: 30884299
Int J Pharm

Enhanced dissolution, permeation and oral bioavailability of aripiprazole mixed micelles: In vitro and in vivo evaluation. [Abstract]

2020 Jun 15;583:119361. PMID: 32334067
CNS Neurosci Ther

Correlation between desynchrony of hippocampal neural activity and hyperlocomotion in the model mice of schizophrenia and therapeutic effects of aripiprazole. [Abstract]

2024 May;30(5):e14739. PMID: 38702935

Aripiprazole purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2024 May;30(5):e14739. [Abstract]

We evaluated the therapeutic effects of Aripiprazole (1 mg/kg, ip, single dose) on the electrophysiological activities of MK‐801‐treated mice.

Aripiprazole purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2024 May;30(5):e14739. [Abstract]

In the MK-801 group, theta power was significantly reduced by Aripiprazole (1 mg/kg, ip, single dose) treatment.

Aripiprazole purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2024 May;30(5):e14739. [Abstract]

The spontaneous spike activity of RS and FS units were significantly reduced by Aripiprazole (1 mg/kg, ip, single dose) treatment in the MK-801 group.
Int J Mol Sci

Differential Effects of Aripiprazole on Electroencephalography-Recorded Gamma-Band Auditory Steady-State Response, Spontaneous Gamma Oscillations and Behavior in a Schizophrenia Rat Model. [Abstract]

2024 Jan 14;25(2):1035. PMID: 38256109

Aripiprazole purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Jan 14;25(2):1035. [Abstract]

Histogram showing the average percentage of change from the vehicle/vehicle-treated group for the PLF of the gamma-band ASSR recorded in rats' global cortex following an acute administration with Aripiprazole (0 and 3 mg/kg) and MK-801 in comparison with vehicle/vehicle-treated animals and MK-801/vehicle-treated animals.

Aripiprazole purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Jan 14;25(2):1035. [Abstract]

Horizontal activity plotted over 240 min following an acute administration with Aripiprazole (Ari) at 1, 3, 10 and 30 mg/kg in MK-801-treated rats in comparison with vehicle (Veh)/vehicle-treated, MK-801/vehicle-treated or MK-801/clozapine (Cloza)-treated rats (clozapine being used as a positive control).
ACS Omega

Involvement of Integrated Stress Response in Drug-Induced Secondary Dystonia. [Abstract]

2025 Oct 17;10(42):50208-50217. PMID: 41179162
Mol Pharmacol

G α Protein Signaling Bias at Serotonin 1A Receptor. [Abstract]

2023 Nov;104(5):230-238. PMID: 37567783
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
Korean J Physiol Pharmacol

Open channel block of Kv1.4 potassium channels by aripiprazole. [Abstract]

2020 Nov 1;24(6):545-553. PMID: 33093275
University of South Carolina

2025.

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (223.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 50 mg/mL (111.51 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

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

2.2302 mL

11.1510 mL

22.3020 mL

5 mM

0.4460 mL

2.2302 mL

4.4604 mL

10 mM

0.2230 mL

1.1151 mL

2.2302 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.58 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.58 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.

Protocol 3

Add each solvent one by one: 10% DMF 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

Protocol 4

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

Solubility: 2.5 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 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)
Instruction de manipulation (2659 KB)

Références

[1]. Burris KD, et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9. [Content Brief]

[2]. Davies MA, et al. Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology. CNS Drug Rev. 2004 Winter;10(4):317-36. [Content Brief]

[3]. Crespo-Facorro B, et al. Aripiprazole as a Candidate Treatment of COVID-19 Identified Through Genomic Analysis. Front Pharmacol. 2021 Mar 2;12:646701. [Content Brief]

[4]. Russo E, et al. Ameliorating effects of aripiprazole on cognitive functions and depressive-like behavior in a genetic rat model of absence epilepsy and mild-depression comorbidity. Neuropharmacology. 2013 Jan;64:371-9. [Content Brief]

[5]. Stip E, et al. Aripiprazole in schizophrenia and schizoaffective disorder: A review. Clin Ther. 2010;32 Suppl 1:S3-20. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMF / DMSO	1 mM	2.2302 mL	11.1510 mL	22.3020 mL	55.7550 mL
	5 mM	0.4460 mL	2.2302 mL	4.4604 mL	11.1510 mL
	10 mM	0.2230 mL	1.1151 mL	2.2302 mL	5.5755 mL
	15 mM	0.1487 mL	0.7434 mL	1.4868 mL	3.7170 mL
	20 mM	0.1115 mL	0.5576 mL	1.1151 mL	2.7878 mL
	25 mM	0.0892 mL	0.4460 mL	0.8921 mL	2.2302 mL
	30 mM	0.0743 mL	0.3717 mL	0.7434 mL	1.8585 mL
	40 mM	0.0558 mL	0.2788 mL	0.5576 mL	1.3939 mL
	50 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1151 mL
	60 mM	0.0372 mL	0.1859 mL	0.3717 mL	0.9293 mL
	80 mM	0.0279 mL	0.1394 mL	0.2788 mL	0.6969 mL
	100 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5576 mL

Keywords

Aripiprazole

11 Cited Publications

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Aripiprazole

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Publications Citing Use of MedChemExpress (MCE) Aripiprazole

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Voir tous les produits spécifiques à Isoform Dopamine Receptor

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Aripiprazole Related Classifications

Cat. No.: HY-14546