product name Palonosetron HCl
Description: Palonosetron HCl (also known as RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. 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).
References: Br J Pharmacol. 1995 Feb;114(4):851-9; Ann Oncol. 2003 Oct;14(10):1570-7.
332.87
Formula
C19H24N2O.HCl
CAS No.
135729-62-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 67 mg/mL (201.3 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
RS 25259, RS 25259 197
other peoduct :
| In Vitro |
In vitro activity: 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). Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Br J Pharmacol. 1995 Feb;114(4):851-9; Ann Oncol. 2003 Oct;14(10):1570-7. |
