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Aripiprazole (OPC-14597)

Alias: OPC-14597; OPC 14597; OPC14597
Cat No.:V0991 Purity: ≥98%
Aripiprazole (formerly OPC-14597; OPC 14597; OPC14597; trade name Abilify) is an approved atypical antipsychotic drug that acts as a high-affinity partial agonist of 5-HT receptor.
Aripiprazole (OPC-14597)
Aripiprazole (OPC-14597) Chemical Structure CAS No.: 129722-12-9
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
500mg
1g
2g
5g
10g
25g
Other Sizes

Other Forms of Aripiprazole (OPC-14597):

  • Aripiprazole D8
  • Aripiprazole (1,1,2,2,3,3,4,4-d8) (Aripiprazole (1,1,2,2,3,3,4,4-d8))
  • Aripiprazole monohydrate (OPC14597)
  • Aripiprazole cavoxil
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Aripiprazole (formerly OPC-14597; OPC 14597; OPC14597; trade name Abilify) is an approved atypical antipsychotic drug that acts as a high-affinity partial agonist of 5-HT receptor. It is a powerful partial agonist at dopamine D2 and 5-HT1A receptors and an antagonist at 5-HT2A receptors, stabilizing the dopamine-serotonin system. Furthermore, aripiprazole has been reported to bind with the antagonist [3H]spiperone and the agonist [125I]7-OH-PIPAT at 0.70±0.22nM and 0.34±0.02nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT1A Receptor ( Ki = 4.2 nM ); 5-HT2A Receptor; 5-HT2B Receptor; 5-HT2C Receptor; D2 Receptor; D3 Receptor; D4 Receptor
ln Vitro

In vitro activity: Aripiprazole exhibits strong binding affinity towards both G protein-coupled and uncoupled receptor states. Aripiprazole strongly stimulates the inhibition of cAMP accumulation mediated by D2 receptors. [1] The dopamine receptors h5-HT(2B), hD(2L) and hD(3) are the ones for which aripiprazole has the highest affinity. However, it also has significant affinity (5-30 nM) for several other 5-HT receptors, including alpha(1A)-adrenergic, hH(1)-histamine, and 5-HT(1A), 5-HT(7). Other G protein-coupled receptors such as the 5-HT(1D), 5-HT(2C), alpha(1B)-, alpha(2A)-, alpha(2B)-, alpha(2C)-, beta(1)-, and beta(2)-adrenergic, and H(3)-histamine receptors are less sensitive to apipirazole (30-200 nM). Aripiprazole functions as a partial agonist at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors in addition to being an inverse agonist at 5-HT(2B) receptors. [2]

ln Vivo
Aripiprazole reduces the levels of extracellular 5-HIAA in the striatum and medial prefrontal cortex of drug-naive rats, but not in rats that have been continuously treated with ripiprazole. [3] Rat hippocampal dopamine release is markedly increased by apiprimeze (0.1 mg/kg and 0.3 mg/kg). The release of dopamine in the medial prefrontal cortex is slightly but significantly increased by apipicazole (0.3 mg/kg), but not in the nucleus accumbens. Dopamine release in the nucleus accumbens is markedly reduced by apipicazole at doses of 3.0 mg/kg and 10 mg/kg, but not in the medical prefrontal cortex. In the medial prefrontal cortex, apipicazole (0.3 mg/kg) momentarily increases the release of dopamine induced by haloperidol (0.1 mg/kg), while inhibiting the release of dopamine in the nucleus accumbens.[4]
Animal Protocol
0.1 mg/kg and 0.3 mg/kg
Rats
References

[1]. J Pharmacol Exp Ther . 2002 Jul;302(1):381-9.

[2]. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.

[3]. Biochem Biophys Res Commun . 1999 Dec 20;266(2):560-3.

[4]. Eur J Pharmacol . 2004 Jun 16;493(1-3):75-83.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H27CL2N3O2
Molecular Weight
448.39
Exact Mass
447.15
Elemental Analysis
C, 61.61; H, 6.07; Cl, 15.81; N, 9.37; O, 7.14
CAS #
129722-12-9
Related CAS #
Aripiprazole-d8; 1089115-06-9; Aripiprazole (1,1,2,2,3,3,4,4-d8); 1089115-04-7; Aripiprazole monohydrate; 851220-85-4; 1259305-26-4 (cavoxil)
Appearance
Solid powder
SMILES
C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
InChi Key
CEUORZQYGODEFX-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H27Cl2N3O2/c24-19-4-3-5-21(23(19)25)28-13-11-27(12-14-28)10-1-2-15-30-18-8-6-17-7-9-22(29)26-20(17)16-18/h3-6,8,16H,1-2,7,9-15H2,(H,26,29)
Chemical Name
7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one
Synonyms
OPC-14597; OPC 14597; OPC14597
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 10~90 mg/mL (22.3~200.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: 2.5 mg/mL (5.58 mM) in 10% DMF 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.


Solubility in Formulation 4: 2.5 mg/mL (5.58 mM) in 10% DMF 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04812379 Active
Recruiting
Drug: Aripiprazole Bipolar Disorder I Otsuka Pharmaceutical Co., Ltd. April 7, 2021 N/A
NCT03522168 Active
Recruiting
Drug: Risperidone
Drug: Aripiprazole
Weight, Body Duke University January 10, 2019 N/A
NCT05531591 Active
Recruiting
Drug: Aripiprazole Augmentation
Drug: Switch to bupropion
Depression
Dementia
Centre for Addiction and
Mental Health
August 1, 2019 Phase 4
NCT05322031 Recruiting Drug: Aripiprazole Schizophrenia
Cognition Disorder
Fondazione IRCCS Ca' Granda,
Ospedale Maggiore Policlinico
January 1, 2022 Phase 4
NCT05545891 Not yet recruiting Drug: Placebo
Drug: Aripiprazole
Dermatillomania
Trichotillomania
(Hair-Pulling Disorder)
University of Chicago December 2023 Phase 2
Biological Data
  • Aripiprazole is a low potency partial agonist at the 5-HT1A receptor stably expressed in 1ACHO cells. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.
  • Effect of aripiprazole on serotonin 5-HT2A receptors. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.
  • Aripiprazole is an inverse agonist at the 5-HT2B receptor in HEK-293 cells. Neuropsychopharmacology . 2003 Aug;28(8):1400-11.
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