Cat. No.: HY-A0019A

Paliperidone palmitate

(Synonyms: 9-Hydroxyrisperidone palmitate)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia.

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

Purity: 99.93%
CAS No.: 199739-10-1
Formula: C₃₉H₅₇FN₄O₄
Molecular Weight:664.89

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Paliperidone palmitate Chemical Structure

CAS No.: 199739-10-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

D₂ Receptor

5-HT_2A Receptor

All Dopamine Receptor Isoforms :

All 5-HT Receptor Isoforms :

In Vivo

Co-administration of paliperidone palmitate (62.4 mg/kg in mice and 20 mg/kg in rats; intramuscular injection; single dose) with hyaluronidase (HY-172442) altered the depot release of paliperidone palmitate in the first 4 days after injection and increased plasma exposure in both BALB/c mice and Sprague Dawley rat models, but did not affect the long-acting release characteristics of paliperidone palmitate. In mice, hyaluronidase altered the tissue morphology at the injection site, resulting in infiltration of macrophages between myocytes, and in rats, granulomas with central cavities and necrosis formed at the injection site[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c mice (female, about 20 g, 6-8 weeks old)+Sprague Dawley rats (male, about 250 g, 6-8 weeks old)^[2]
Dosage:

Mice: 62.4 mg/kg of Paliperidone palmitate, 5 U or 15 U of hyaluronidase (dissolved in normal saline)
Rats: 20 mg/kg of Paliperidone palmitate, 5 U or 15 U of Hyaluronidase (dissolved in phosphate buffered saline)
Administration:

Intramuscular injection, single dose; for mice, 4-week study period; for rats, 21-28-day study period
Result:

In mice, co-administration of hyaluronidase increased paliperidone plasma exposures in the first week after injection. The overall long-acting release nature of the formulation was maintained. Macrophages showed infiltration between individual myocytes when paliperidone palmitate was co-administered with hyaluronidase.
In rats, co-administration of hyaluronidase also increased exposure in the first 4 days, but the effect was less than that in mice. The long-acting exposure was still maintained for about 20 days. Co-administration of hyaluronidase did not discernably affect the granulomas or the surrounding myocytes in rats. The lymph node retention of paliperidone palmitate was diminished upon treatment with hyaluronidase in both mice and rats. The biphasic plasma concentration-time profiles of paliperidone in both species could be described by an open first-order disposition model with parallel fast and slow absorption processes.
The macrophage infiltration and angiogenesis at the injection site affected the drug release and absorption, and the effect of hyaluronidase on these processes was different between mice and rats.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 199739-10-1
Appearance Solid
Molecular Weight 664.89
Formula C₃₉H₅₇FN₄O₄
Color White to off-white
SMILES

O=C(OC1CCCN(C1=NC(C)=C2CCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)C2=O)CCCCCCCCCCCCCCC
Synonyms

9-Hydroxyrisperidone palmitate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (1)

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Journal Impact Factor

Int J Pharm

Impact of macrophages on the dissolution of LAI suspension prodrugs. [Abstract]

2026 Mar 7:126762. PMID: 41802501

Solvent & Solubility

In Vitro:

Ethanol : 2 mg/mL (3.01 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5040 mL

7.5200 mL

15.0401 mL

5 mM

---

10 mM

---

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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Darville N, et al. The effect of macrophage and angiogenesis inhibition on the drug release and absorption from an intramuscular sustained-release paliperidone palmitate suspension. J Control Release. 2016 May 28;230:95-108. [Content Brief]

[2]. Pertinez H, et al. Hyaluronidase impacts exposures of long-acting injectable paliperidone palmitate in rodent models. bioRxiv [Preprint]. 2024 Mar 6:2024.03.03.583160. [Content Brief]

[3]. Kwon JS, et al. Satisfaction of immediate or delayed switch to paliperidone palmitate in patients unsatisfied with current oral atypical antipsychotics. Int Clin Psychopharmacol. 2015;30(6):320-328. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol	1 mM	1.5040 mL	7.5200 mL	15.0401 mL	37.6002 mL

Keywords

Paliperidone palmitate

1 Cited Publications

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Paliperidone palmitate

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Publications Citing Use of MedChemExpress (MCE) Paliperidone palmitate

All Dopamine Receptor Isoforms

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Paliperidone palmitate Related Classifications

Cat. No.: HY-A0019A