Home Neuronal Signaling 5-HT Receptor antagonist Palonosetron HCl

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Palonosetron HCl 5-HT Receptor antagonist

Cat.No.S3050

Palonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
Palonosetron HCl 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 332.87

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Chemical Information, Storage & Stability

Molecular Weight 332.87 Formula

C19H24N2O.HCl

 Storage (From the date of receipt)
CAS No. 135729-62-3 Download SDF Storage of Stock Solutions

Synonyms RS 25259, RS 25259 197 Smiles C1CC2CN(C(=O)C3=CC=CC(=C23)C1)C4CN5CCC4CC5.Cl

Solubility

In vitro
Batch:

Water : 67 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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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.
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Mechanism of Action

Targets/IC50/Ki
5-HT3 [1]
In vitro
Palonosetron is a highly potent, selective, second-generation 5-HT3 receptor antagonist with a 5-HT3 receptor binding affinity that is ∼100-fold higher than other 5-HT3 receptor antagonists (pKi 10.5 compared with 8.91 for granisetron, 8.81 for tropisetron, 8.39 for ondansetron, 7.6 for dolasetron). Palonosetron also has an extended plasma elimination half-life of ∼40 h, significantly longer than others in its class (ondansetron, 4 h; tropisetron, 7.3 h; dolasetron, 7.5 h; ranisetron, 8.9 h).
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

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