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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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

Water : 67 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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In vivo
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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

Mechanism of Action

Targets/IC50/Ki
5-HT3
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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