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(R,R)-Palonosetron Hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(R,R)-Palonosetron Hydrochloride图片
CAS NO:135729-75-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)332.87
FormulaC19H24N2O.HCl
CAS No.135729-75-8
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
SMILESO=C1N([C@@H]2CN3CCC2CC3)C[C@@]4([H])C5=C1C=CC=C5CCC4.[H]Cl
Synonyms(R,R)-RS 25259, RS-25233-197; RS25233-198; RS 25259 197; RS 25233-197; (R,R)-RS25233-197; RS-25233-198; RS 25233-198; RS-25259-197; (R,R)-Palonosetron hydrochloride; US brand name: Aloxi and Akynzeo
实验参考方法
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: 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).


Cell Assay: Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). IC50 Value: Target: 5-HT3 Receptor Palonosetron is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy.

In Vivo
Animal model
Formulation & Dosage
ReferencesBr J Pharmacol. 1995 Feb;114(4):851-9; Ann Oncol. 2003 Oct;14(10):1570-7.