Palonosetron HCl

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03817970 Not yet recruiting Nephrotoxicity University of Colorado Denver|Memorial Sloan Kettering Cancer Center|Rutgers University|National Institute of General Medical Sciences (NIGMS) April 25 2019 Not Applicable
NCT03817970 Not yet recruiting Nephrotoxicity University of Colorado Denver|Memorial Sloan Kettering Cancer Center|Rutgers University|National Institute of General Medical Sciences (NIGMS) April 25 2019 Not Applicable
NCT03586817 Recruiting Nausea and Vomiting Postoperative Hospital Federal de Bonsucesso March 2 2019 Phase 4
NCT03586817 Recruiting Nausea and Vomiting Postoperative Hospital Federal de Bonsucesso March 2 2019 Phase 4
NCT03649230 Recruiting Chemotherapy-Induced Nausea and Vomiting Purdue Pharma Canada October 3 2018 --
NCT03578081 Recruiting Malignant Neoplasm Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) October 15 2018 Phase 3

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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