Name: Paliperidone
Brand: Selleck Chemicals
SKU: S1724
Availability: InStock
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Dopamine Receptor Inhibitors	MPTP Hydrochloride Trifluoperazine Trifluoperazine 2HCl Penfluridol SCH-23390 hydrochloride Domperidone SKF38393 HCl Sulpiride Azaperone C-DIM12

Solubility

In vitro
Batch:

5%TFA : 15 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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

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%

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.

Chemical Information, Storage & Stability

Molecular Weight	426.48	Formula	C₂₃H₂₇FN₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	144598-75-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

Mechanism of Action

Targets/IC₅₀/Ki	Dopamine receptor
In vitro	Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. This compound works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protects SH-SY5Y from hydrogen peroxide. It completely diminishes cell reduction induced by different stressors, regardless of their dosages. This chemical is demonstrated with higher oxidative stress-scavenging properties than other APDs in several aspects, such as generated bulk glutathione, low HNE, and protein carbonyl productions. It enhances dopamine toxicity at the highest dose and is the only AP that significantly increases cell viability (8.1%) compared with cells treated with dopamine alone.
In vivo	Paliperidone normalizes prefrontal cortical basal extracellular glutamate in rats. This compound also prevents the acute MK-801-induced increase in extracellular glutamate in rats. When coadministered with Escitalopram, it restores the suppression of the NE neuronal firing rate (n = 5 rats) and the percentage of neurons exhibiting burst firing. It results in a dose-dependent decrease in bite and attack behaviors with an effective dose. This chemical results in the maximal reduction in aggressive behavior.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16936711/ [2] https://pubmed.ncbi.nlm.nih.gov/21523348/ [3] https://pubmed.ncbi.nlm.nih.gov/21878360/ [4] https://pubmed.ncbi.nlm.nih.gov/21699956/ [5] https://pubmed.ncbi.nlm.nih.gov/17530476/ [6] https://pubmed.ncbi.nlm.nih.gov/19066856/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06060886	Not yet recruiting	Schizophrenia\|Treatment-resistant Schizophrenia\|Side Effect\|Lipid Metabolism Disorders\|Diabetes\|NAFLD\|Psychosis	Consorcio Centro de Investigación Biomédica en Red (CIBER)\|Instituto de Salud Carlos III	November 1 2023	Phase 4
NCT02532842	Completed	Schizophrenia	Janssen Pharmaceutica N.V. Belgium	July 2015	--
NCT01584466	Withdrawn	Schizophrenia	University of Maryland Baltimore	January 2014	Not Applicable

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Paliperidone Dopamine Receptor antagonist

Chemical Structure

Molecular Weight: 426.48