Palonosetron HCl

For research use only.

Catalog No.S3050 Synonyms: RS 25259, RS 25259 197

Palonosetron HCl Chemical Structure

Molecular Weight(MW): 332.87

Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.

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Biological Activity

Description Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
Targets
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).

Protocol

Solubility (25°C)

In vitro Water 67 mg/mL (201.27 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 332.87
Formula

C19H24N2O.HCl

CAS No. 135729-62-3
Storage powder
in solvent
Synonyms RS 25259, RS 25259 197
Smiles Cl.O=C1N(CC2CCCC3=CC=CC1=C23)C4CN5CCC4CC5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03148704 Unknown status Drug: palonosetron hydrochloride capsules Palonosetron Cttq March 8 2017 --
NCT00982995 Terminated Drug: Palonosetron Nausea|Vomiting|Terminally Ill University of Michigan Rogel Cancer Center November 2010 Phase 2
NCT01074697 Completed Drug: Fosaprepitant dimeglumine|Drug: Placebo Nausea|Vomiting|Genital Neoplasms Female Odense University Hospital|Helsinn Healthcare SA April 2010 Phase 3
NCT01046240 Completed Drug: Palonosetron Emesis Clinica Universidad de Navarra Universidad de Navarra October 2009 Phase 1|Phase 2
NCT00869973 Terminated Drug: Aprepitant|Drug: dexamethasone Emesis S. Maria Hospital Terni September 2009 Phase 3

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.

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID