Choose Your Country or Region

Aripiprazole

Name: Aripiprazole
Brand: Selleck Chemicals
SKU: S1975
Rating: 5 (8 reviews)

Catalog No.S1975 Synonyms: OPC-14597

For research use only.

Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

CAS No. 129722-12-9

Selleck's Aripiprazole has been cited by 8 Publications

2 Customer Reviews

Purity & Quality Control

Choose Selective 5-HT Receptor Inhibitors

Related Compound Libraries

Other 5-HT Receptor Products

AZD3839^New

AZD3839 is a potent and selective BACE1 inhibitor with K_i of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
Xanthohumol^New

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.
Nirogacestat (PF-03084014)^New

Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.
Fluoxetine (Lilly 110140) HCl

Fluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.
WAY-100635 Maleate

WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.
Ketanserin

Ketanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with K_i of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.
Asenapine maleate

Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Iloperidone

Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
Duloxetine HCl

Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with K_i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
Risperidone

Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

Download Inhibitor Catalog

5-HT Receptor Signaling Pathway Map

Biological Activity

Description

Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

Targets

5-HT1A ^[1]

4.2 nM(Ki)

In vitro

Aripiprazole binds with high affinity to both the G protein-coupled and uncoupled states of receptors. Aripiprazole potently activates D2 receptor-mediated inhibition of cAMP accumulation. ^[1] Aripiprazole has highest affinity for h5-HT(2B)-, hD(2L)-, and hD(3)-dopamine receptors, but also has significant affinity (5-30 nM) for several other 5-HT receptors (5-HT(1A), 5-HT(2A), 5-HT(7)), as well as alpha(1A)-adrenergic and hH(1)-histamine receptors. Aripiprazole has less affinity (30-200 nM) for other G protein-coupled receptors, including 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. Aripiprazole is an inverse agonist at 5-HT(2B) receptors and displays partial agonist actions at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors. ^[2]

In vivo

Aripiprazole reduces extracellular 5-HIAA concentrations in the medial prefrontal cortex and striatum of drug-naive rats, but not in chronic Aripiprazole-pretreated rats. ^[3] Aripiprazole, 0.1 mg/kg and 0.3 mg/kg, significantly increases dopamine release in the hippocampus of rats. Aripiprazole, 0.3 mg/kg, slightly but significantly increases dopamine release in the medial prefrontal cortex but not in the nucleus accumbens. Aripiprazole, 3.0 mg/kg and 10 mg/kg, significantly decreases dopamine release in the nucleus accumbens but not the medical prefrontal cortex. Aripiprazole, 0.3 mg/kg, transiently potentiates haloperidol (0.1 mg/kg)-induced dopamine release in the medial prefrontal cortex but inhibited that in the nucleus accumbens. ^[4]

Protocol (from reference)

References

[4] Li Z, et al. Eur J Pharmacol, 2004, 493(1-3), 75-83.

+ Expand

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	448.39
Formula	C₂₃H₂₇Cl₂N₃O₂
CAS No.	129722-12-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl

Download Aripiprazole SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05322031	Recruiting	Drug: Aripiprazole	Schizophrenia\|Myelin Degeneration\|Cognition Disorder	Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico	January 1 2022	Phase 4
NCT04907279	Recruiting	Drug: Aripiprazole Once-Monthly (AOM)	Schizophrenia\|Schizo Affective Disorder\|Bipolar I Disorder	Otsuka Canada Pharmaceutical Inc.\|Lundbeck Canada Inc.	November 1 2021	--
NCT04030143	Completed	Drug: Aripiprazole	Schizophrenia\|Bipolar I Disorder	Otsuka Pharmaceutical Development & Commercialization Inc.\|PRA Health Sciences	July 31 2019	Phase 1\|Phase 2
NCT03881449	Unknown status	Combination Product: ABILIFY MYCITE	Schizophrenia\|Major Depressive Disorder\|Bi-Polar Disorder\|Schizo Affective Disorder	Durham VA Medical Center\|Otsuka Pharmaceutical Development and Commercialization Inc.	April 4 2019	Phase 4
NCT03854409	Completed	Drug: Aripiprazole	Schizophrenia\|Bipolar I Disorder	Otsuka Pharmaceutical Development & Commercialization Inc.\|PRA Health Sciences\|H. Lundbeck A/S	January 31 2019	Phase 1
NCT03342963	Completed	Drug: ASC-01\|Drug: Aripiprazole and sertraline	Healthy Male Adults	Otsuka Pharmaceutical Co. Ltd.	November 21 2017	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):