Paliperidone Palmitate | CAS#199739-10-1| MedKoo

MedKoo Cat#: 341424 | Name: Paliperidone Palmitate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class of medications. It is developed by Janssen Pharmaceutica. Invega is an extended release formulation of paliperidone that uses the OROS extended release system to allow for once-daily dosing.Paliperidone has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors. It does not bind to muscarinic acetylcholine receptors. In addition, it binds with dopamine and serotonin receptors.

Chemical Structure

Paliperidone Palmitate

CAS#199739-10-1

Theoretical Analysis

MedKoo Cat#: 341424

Name: Paliperidone Palmitate

CAS#: 199739-10-1

Chemical Formula: C39H57FN4O4

Exact Mass: 664.4364

Molecular Weight: 664.91

Elemental Analysis: C, 70.45; H, 8.64; F, 2.86; N, 8.43; O, 9.62

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

Paliperidone Palmitate; RO 92670; RO-92670; RO92670.

IUPAC/Chemical Name

Hexadecanoic acid, 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl)-6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido(1,2-a)pyrimidin-9-yl ester

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

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 664.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Joshi K, Muser E, Xu Y, Schwab P, Datar M, Suehs B. Adherence and economic impact of paliperidone palmitate versus oral atypical antipsychotics in a Medicare population. J Comp Eff Res. 2018 May 3. doi: 10.2217/cer-2018-0003. [Epub ahead of print] PubMed PMID: 29722547. 2: Deslandes PN, Ward EH, Norris K, Sewell RD. Effectiveness of paliperidone long-acting injection in clinical practice. Ther Adv Psychopharmacol. 2018 May;8(5):139-145. doi: 10.1177/2045125317753332. Epub 2018 Jan 17. PubMed PMID: 29713451; PubMed Central PMCID: PMC5896863. 3: Russu A, Kern Sliwa J, Ravenstijn P, Singh A, Mathews M, Kim E, Gopal S. Maintenance dose conversion between oral risperidone and paliperidone palmitate 1 month: Practical guidance based on pharmacokinetic simulations. Int J Clin Pract. 2018 Apr 30:e13089. doi: 10.1111/ijcp.13089. [Epub ahead of print] PubMed PMID: 29707876. 4: Jukic V, Jakovljevic M, Filipcic I, Herceg M, Silic A, Tomljanovic T, Zilbershtein R, Jensen RCD, Hemels MEH, Einarson TR. Cost-Utility Analysis of Depot Atypical Antipsychotics for Chronic Schizophrenia in Croatia. Value Health Reg Issues. 2013 Sep - Oct;2(2):181-188. doi: 10.1016/j.vhri.2013.06.008. Epub 2013 Sep 13. PubMed PMID: 29702863. 5: Augusto M, Greene M, Touya M, Sweeney SM, Waters H. Cost-effectiveness of long-acting injectable aripiprazole once-monthly 400 mg in bipolar I disorder in the USA. J Comp Eff Res. 2018 Apr 25. doi: 10.2217/cer-2018-0010. [Epub ahead of print] PubMed PMID: 29694244. 6: Augusto M, Greene M, Touya M, Sweeney SM, Waters H. Budget impact analysis of long-acting injectable aripiprazole once-monthly 400 mg in bipolar I disorder in the USA. J Comp Eff Res. 2018 Apr 25. doi: 10.2217/cer-2018-0009. [Epub ahead of print] PubMed PMID: 29694243. 7: Tagne Nouemssi AB. Risperidone-associated sinus tachycardia potentiated by paliperidone palmitate in a patient with no prior cardiovascular disease: role of risperidone-related autonomic instability. BMJ Case Rep. 2018 Apr 21;2018. pii: bcr-2017-221771. doi: 10.1136/bcr-2017-221771. PubMed PMID: 29680794. 8: Patel H, Patel P, Modi N, Patel P, Wagh Y, George A, Desai N, Srinivas NR. Rats and rabbits as pharmacokinetic screening tools for long acting intramuscular depots: Case study with paliperidone palmitate suspension. Xenobiotica. 2018 Apr 12:1-24. doi: 10.1080/00498254.2018.1464683. [Epub ahead of print] PubMed PMID: 29642738. 9: Li N, Feng Y, Lu H, Cai SL, Zhuo J, Si T, Zhang L. Factors related to improvement of symptoms, function, and caregiver burden in Chinese patients with schizophrenia after switching to paliperidone palmitate once-monthly from oral antipsychotics. Neuropsychiatr Dis Treat. 2018 Mar 22;14:825-837. doi: 10.2147/NDT.S158353. eCollection 2018. PubMed PMID: 29606876; PubMed Central PMCID: PMC5868613. 10: Lee CJ, Lan TH, Tsai CJ. Paliperidone palmitate treatment in a patient with monosomy X karyotype Turner syndrome who later developed schizophrenia. Psychiatry Clin Neurosci. 2018 Mar 30. doi: 10.1111/pcn.12657. [Epub ahead of print] PubMed PMID: 29603521. 11: Jann MW, Penzak SR. Long-Acting Injectable Second-Generation Antipsychotics: An Update and Comparison Between Agents. CNS Drugs. 2018 Mar;32(3):241-257. doi: 10.1007/s40263-018-0508-6. Review. PubMed PMID: 29569082. 12: Ceskova E, Silhan P. Novel treatment options in depression and psychosis. Neuropsychiatr Dis Treat. 2018 Mar 13;14:741-747. doi: 10.2147/NDT.S157475. eCollection 2018. Review. PubMed PMID: 29559781; PubMed Central PMCID: PMC5856289. 13: Tompsett T, Masters K, Donyai P. The utility of novel outcome measures in a naturalistic evaluation of schizophrenia treatment. Neuropsychiatr Dis Treat. 2018 Mar 2;14:681-691. doi: 10.2147/NDT.S151174. eCollection 2018. PubMed PMID: 29535524; PubMed Central PMCID: PMC5841343. 14: Singh A, Gopal S, Kim E, Mathews M, Kern-Sliwa J, Turkoz I, Wooller A, Berlin J. Methodological challenges in indirect treatment comparisons: spotlight on a recent comparison of long-acting injectable aripiprazole versus paliperidone palmitate in the treatment of schizophrenia. Int Clin Psychopharmacol. 2018 Mar 1. doi: 10.1097/YIC.0000000000000215. [Epub ahead of print] PubMed PMID: 29494348. 15: Theodoros T, Taylor M, Huang HC, Wang N, Motamarri B. Going the distance: reviewing antipsychotic depot or long-acting injectable treatments in Australasia. Australas Psychiatry. 2018 Feb 1:1039856218758559. doi: 10.1177/1039856218758559. [Epub ahead of print] PubMed PMID: 29457473. 16: Kamstra R, Pilon D, Lefebvre P, Emond B, Joshi K. Treatment patterns and Medicaid spending in comorbid schizophrenia populations: once-monthly paliperidone palmitate versus oral atypical antipsychotics. Curr Med Res Opin. 2018 Feb 28:1-12. doi: 10.1080/03007995.2018.1442822. [Epub ahead of print] PubMed PMID: 29452492. 17: Kern Sliwa J, Savitz A, Nuamah I, Mathews M, Gopal S, Elefant E, Najarian D, Alphs L. An assessment of injection site reaction and injection site pain of 1-month and 3-month long-acting injectable formulations of paliperidone palmitate. Perspect Psychiatr Care. 2018 Feb 14. doi: 10.1111/ppc.12267. [Epub ahead of print] PubMed PMID: 29446084. 18: Geerts H, Spiros A, Roberts P, Alphs L. A quantitative systems pharmacology study on optimal scenarios for switching to paliperidone palmitate once-monthly. Schizophr Res. 2018 Jan 25. pii: S0920-9964(17)30711-9. doi: 10.1016/j.schres.2017.11.016. [Epub ahead of print] PubMed PMID: 29395607. 19: Çayköylü A, Karslıoğlu EH, Özer İ, Köksal AG. Hypersexuality associated with paliperidone. Exp Clin Psychopharmacol. 2018 Apr;26(2):109-112. doi: 10.1037/pha0000178. Epub 2018 Feb 1. PubMed PMID: 29389211. 20: Fortea A, Ilzarbe D, Espinosa L, Solerdelcoll M, de Castro C, Oriolo G, Sugranyes G, Baeza I. Long-Acting Injectable Atypical Antipsychotic Use in Adolescents: An Observational Study. J Child Adolesc Psychopharmacol. 2018 Jan 30. doi: 10.1089/cap.2017.0096. [Epub ahead of print] PubMed PMID: 29381388.