Paliperidone

Alias:
Cat No.:V1260 Purity: ≥98%
Paliperidone (Invega; Invega Sustenna; Invega Sustenna; 9-hydroxyrisperidone), the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist used for the treatment of schizophrenia.
Paliperidone Chemical Structure CAS No.: 144598-75-4
Product category: Dopamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Paliperidone:

  • Paliperidone-d4 (Paliperidone d4)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Paliperidone (Invega; Invega Sustenna; Invega Sustenna; 9-hydroxyrisperidone), the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist used for the treatment of schizophrenia. Paliperidone works in a concentration-dependent manner by significantly increasing the intracellular accumulation of Rh123 and DOX. Paliperidone has outperformed other APDs in a number of oxidative stress-scavenging metrics, including produced glutathione in bulk, low HNE, and protein carbonyl production.

Biological Activity I Assay Protocols (From Reference)
Targets
α2 adrenergic receptor; α1 adrenergic receptor; α adrenergic receptor; 5-HT2A Receptor; D2 Receptor
ln Vitro

In vitro activity: Paliperidone raises Rh123 and DOX intracellular accumulation considerably in a concentration-dependent way.[1] Paliperidone exclusively shields SH-SY5Y from hydrogen peroxide and functions well at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+). Regardless of the dosage, paliperidone (100 μM) completely mitigates cell reduction caused by various stressors. In comparison to other APDs, paliperidone is shown to have better oxidative stress-scavenging abilities in a number of areas, including produced bulk glutathione, low HNE, and protein carbonyl productions.[2] The only AP that considerably raises cell viability (8.1%) when compared to cells treated with dopamine alone is paliperidone, which also increases dopamine toxicity at the highest dosage.[3]

ln Vivo
Paliperidone brings basal extracellular glutamate in the prefrontal cortex back to normal in rats. Additionally, paliperidone keeps rats' extracellular glutamate levels from rising sharply in response to MK-801.[4] The percentage of neurons exhibiting burst firing and the suppression of the NE neuronal firing rate (n = 5 rats) are restored when paliperidone and escitalopram are administered together.[5] When paliperidone is used at an effective dose, bite and attack behaviors decrease in a dose-dependent manner. The most significant decrease in aggressive behavior is observed with paliperidone.[6]
Animal Protocol
N/A
Rats
References

[1]. Neuropsychopharmacology . 2007 Apr;32(4):757-64.

[2]. Psychopharmacology (Berl) . 2011 Oct;217(3):397-410.

[3]. Prog Neuropsychopharmacol Biol Psychiatry . 2012 Jan 10;36(1):71-7.

[4]. Neurosci Lett . 2011 Aug 18;500(3):167-71.

[5]. Psychopharmacology (Berl) . 2007 Sep;194(1):63-72.

[6]. Psychopharmacology (Berl) . 2009 May;203(4):653-63.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H27FN4O3
Molecular Weight
426.48
Exact Mass
426.21
Elemental Analysis
C, 64.77; H, 6.38; F, 4.45; N, 13.14; O, 11.25
CAS #
144598-75-4
Related CAS #
Paliperidone-d4; 1020719-55-4
Appearance
Solid powder
SMILES
CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F
InChi Key
PMXMIIMHBWHSKN-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3
Chemical Name
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
Synonyms

9-Hydroxyrisperidone; Invega; Paliperidone; 9-OH-risperidone; Invega Sustenna; Invega Sustenna; paliperidone

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

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: 4~5 mg/mL (9.4~11.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.17 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 5.0 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: ≥ 0.5 mg/mL (1.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

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Solubility in Formulation 3: ≥ 0.5 mg/mL (1.17 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 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3448 mL 11.7239 mL 23.4478 mL
5 mM 0.4690 mL 2.3448 mL 4.6896 mL
10 mM 0.2345 mL 1.1724 mL 2.3448 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

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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:
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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
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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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
NCT04940039 Active
Recruiting
Drug: Risperidone 3 mg
Drug: Paliperidone Palmitate
50 mg eq.
Schizophrenia Janssen-Cilag International NV July 22, 2021 Phase 4
NCT03485417 Recruiting Drug: Paliperidone
Drug: Aripiprazole
Stimulant Abuse
Pharmacotherapy
The University of Hong Kong June 1, 2019 Phase 2
Phase 3
NCT06060886 Not yet recruiting Drug: Aripiprazole
Drug: Paliperidone
Schizophrenia
Diabetes
Consorcio Centro de
Investigación Biomédica en Red
(CIBER)
November 1, 2023 Phase 4
NCT01399450 Completed Drug: paliperidone Schizophrenia Seoul National University
Hospital
August 2011 Phase 4
NCT00761605 Completed Drug: Paliperidone Schizophrenia Janssen Korea, Ltd., Korea April 2008 Phase 4
Biological Data
  • Paliperidone
    Effect of risperidone and paliperidone on basal extracellular glutamate in prefrontal cortex of saline- and polyI:C-treated offspring:Neurosci Lett.2011 Aug 18;500(3):167-71.
  • Paliperidone
    Risperidone and paliperidone suppress MK-801-induced extracellular glutamate elevation.Neurosci Lett.2011 Aug 18;500(3):167-71.
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