Aripiprazole (Synonyms: OPC-14597)

Name: Aripiprazole
Brand: MedChemExpress
SKU: HY-14546
Rating: 5.0 (8 reviews)

Cat. No.: HY-14546 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Aripiprazole Chemical Structure

CAS No. : 129722-12-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 86	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 86	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 139	In-stock	Estimated Time of Arrival: December 31
1 g	USD 178	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Aripiprazole:

Aripiprazole-d₈ Get quote
Aripiprazole monohydrate Get quote
Aripiprazole (1,1,2,2,3,3,4,4-d₈) Get quote
Aripiprazole (Standard) Get quote

8 Publications Citing Use of MCE Aripiprazole

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT_1A Receptor

4.2 nM (Ki)

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

D₂ Receptor

D₃ Receptor

D₄ 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	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	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 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	> 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	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	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	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.

Clinical Trial

Molecular Weight

448.39

Formula

C₂₃H₂₇Cl₂N₃O₂

CAS No.

129722-12-9

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

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).

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

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: 99.95%

Select Batch:

Data Sheet (277 KB) SDS (394 KB)

COA (251 KB) HNMR (271 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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]

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

Aripiprazole Related Classifications

Neurological Disease Inflammation/Immunology Infection

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:

Aripiprazole129722-12-9OPC-14597OPC14597OPC 145975-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorCHO-D2L cellsAntipsychoticDopamineSerotoninPrefrontal cortexHippocampusCOVID19Inhibitorinhibitorinhibit

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Aripiprazole (Synonyms: OPC-14597)

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Other Forms of Aripiprazole:

Aripiprazole Related Antibodies

8 Publications Citing Use of MCE Aripiprazole

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Purity & Documentation

References

Customer Review

Aripiprazole Related Antibodies

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Complete Stock Solution Preparation Table

Aripiprazole Related Classifications

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