| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Paliperidone palmitate (RO-92670; 9-Hydroxyrisperidone palmitate; RO92670) is a novel and potent dopamine antagonist and 5-HT2A antagonist that belongs to the atypical antipsychotic class of medications. Paliperidone exhibits antagonistic effects on H1 histamine receptors as well as α1 and α2 adrenergic receptors. Muscarinic acetylcholine receptors are not bound by it. Furthermore, it binds to serotonin and dopamine receptors. In a concentration-dependent manner, paliperidone markedly increases the intracellular accumulation of Rh123 and DOX. In comparison to other APDs, paliperidone has shown better oxidative stress-scavenging abilities in a number of areas, including produced bulk glutathione, low HNE, and protein carbonyl production.
| Targets |
5-HT2A Receptor; D2 Receptor
|
|---|---|
| ln Vitro |
In vitro activity: Paliperidone dramatically increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. 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. 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.
|
| ln Vivo |
Paliperidone restores basal extracellular glutamate in the prefrontal cortex in rats. Additionally, in rats, paliperidone inhibits the acute increase in extracellular glutamate induced by MK-801. When paliperidone and escitalopram are taken together, the suppression of the percentage of neurons exhibiting burst firing and the NE neuronal firing rate (n = 5 rats) is restored. At an effective dosage, paliperidone reduces bite and attack behaviors in a dose-dependent manner. Paliperidone gives rise to the greatest possible decrease in aggressive conduct.
|
| Animal Protocol |
Rats
|
| References |
[2]. J Comp Eff Res. 2018 May 3. doi: 10.2217/cer-2018-0003. |
| Molecular Formula |
C39H57FN4O4
|
|---|---|
| Molecular Weight |
664.89268
|
| Exact Mass |
664.44
|
| Elemental Analysis |
C, 70.45; H, 8.64; F, 2.86; N, 8.43; O, 9.62
|
| CAS # |
199739-10-1
|
| Related CAS # |
144598-75-4; 199739-10-1 (palmitate)
|
| Appearance |
Solid powder
|
| SMILES |
CCCCCCCCCCCCCCCC(=O)OC1CCCN2C1=NC(=C(C2=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F)C
|
| InChi Key |
VOMKSBFLAZZBOW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C39H57FN4O4/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-18-36(45)47-34-17-16-24-44-38(34)41-29(2)32(39(44)46)23-27-43-25-21-30(22-26-43)37-33-20-19-31(40)28-35(33)48-42-37/h19-20,28,30,34H,3-18,21-27H2,1-2H3
|
| Chemical Name |
[3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl] hexadecanoate
|
| Synonyms |
RO 92670; RO92670; RO-92670; Paliperidone Palmitate
|
| 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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~1 mg/mL (~1.5 mM)
Ethanol: ~2 mg/mL (~3.0 mM) |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5040 mL | 7.5200 mL | 15.0401 mL | |
| 5 mM | 0.3008 mL | 1.5040 mL | 3.0080 mL | |
| 10 mM | 0.1504 mL | 0.7520 mL | 1.5040 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.
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.
| 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 |
| NCT01860781 | Completed | Drug: paliperidone palmitate | Schizophrenia | Seoul National University Hospital |
August 2011 | Phase 4 |
| NCT01682161 | Completed | Drug: Paliperidone palmitate | Schizophrenia | Janssen Korea, Ltd., Korea | January 2012 | Phase 4 |
| NCT01258920 | Completed | Drug: Paliperidone palmitate | Schizophrenia | Janssen Pharmaceutical K.K. | October 2010 | Phase 3 |
| NCT01685931 | Completed | Drug: Paliperidone Palmitate | Schizophrenia | Xian-Janssen Pharmaceutical Ltd. | November 2012 | Phase 4 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA