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Palonosetron

Name: Palonosetron
Brand: Selleck Chemicals
SKU: S5740

Synonyms: RS25259, RS 25259 197

Catalog No.S5740 Purity: 99%

Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

Palonosetron Chemical Structure

CAS: 135729-61-2

Purity & Quality Control

Batch: S574001 DMSO] 59 mg/mL] false] ] ] false] ] ] false Purity: 99%

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Biological Activity

Description

Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

Targets

5-HT3 receptor ^[2]

0.17 nM(Ki)

In vitro
In vitro	Palonosetron is a 5-HT3 receptor antagonist with a high binding affinity for this receptor and little or no affinity for other receptors^[1].

In Vivo
In vivo	Palonosetron has a longer half-life and a higher binding affinity than the first-generation 5-HT3 receptor antagonists. After intravenous dosing of palonosetron in healthy subjects and cancer patients, an initial decline in plasma concentration is followed by a slow elimination from the body. Mean maximum plasma concentration and area under the concentration-time curves are generally dose-proportional over the dose range of 0.3 to 90 μg/kg in healthy subjects and in cancer patients. Palonosetron has a volume of distribution of approximately 8.3 ± 2.5 L/kg and is 62% bound to plasma proteins. It is eliminated from the body through renal excretion and metabolic pathways. The mean terminal elimination half-life is approximately 40 hours^[1].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04486157	Completed	Healthy	HK inno.N Corporation	March 18 2021	Phase 1
NCT04466046	Completed	Postoperative Nausea and Vomiting	Daegu Catholic University Medical Center	September 4 2019	--
NCT03148704	Unknown status	Palonosetron	Cttq	March 8 2017	--
NCT00982995	Terminated	Nausea\|Vomiting\|Terminally Ill	University of Michigan Rogel Cancer Center	November 2010	Phase 2
NCT01074697	Completed	Nausea\|Vomiting\|Genital Neoplasms Female	Odense University Hospital\|Helsinn Healthcare SA	April 2010	Phase 3

References

Chemical lnformation & Solubility

Molecular Weight	296.41	Formula	C₁₉H₂₄N₂O
CAS No.	135729-61-2	SDF	--
Smiles	C1CC2CN(C(=O)C3=CC=CC(=C23)C1)C4CN5CCC4CC5
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 59 mg/mL ( (199.04 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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Molarity Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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