(R,R)-Palonosetron Hydrochloride

Molecular Weight (MW)	332.87
Formula	C19H24N2O.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
SMILES	O=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

Molecular Weight (MW)

332.87

Formula

C19H24N2O.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

SMILES

O=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

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
References	Br J Pharmacol. 1995 Feb;114(4):851-9; Ann Oncol. 2003 Oct;14(10):1570-7.

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

References

Br J Pharmacol. 1995 Feb;114(4):851-9; Ann Oncol. 2003 Oct;14(10):1570-7.

CAS NO:	135729-75-8
规格:	≥98%

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