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    Palonosetron HCl (RS25233-197; Aloxi)
    Palonosetron HCl (RS25233-197; Aloxi)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1022
    CAS #: 135729-62-3Purity ≥98%

    Description: Palonosetron HCl (formerly RS-25259, RS-25259, RS 25259 197, RS-25259197; trade names: Aloxi and Akynzeo), an approved antiemetic drug, is a potent 5-HT3 antagonist that has been used in the prevention and treatment of chemotherapy-induced nausea and vomiting. As of April 2018, the combination of fosnetupitant and palonosetron has been approved by FDA to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. 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.

    Related CAS: 135729-61-2 (free base); 135729-75-8 ((R,R)-Palonosetron Hydrochloride)

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    Molecular Weight (MW)332.87 
    FormulaC19H24N2O.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
    SMILESO=C1N([[email protected]@H]2CN3CCC2CC3)C[[email protected]@]4([H])C5=C1C=CC=C5CCC4.[H]Cl
    SynonymsRS-25233-197; RS25233-198; RS 25259, RS 25259 197; Palonosetron hydrochloride; RS 25233-197; RS25233-197; RS-25233-198; RS 25233-198; RS-25259-197; US brand name: Aloxi and Akynzeo


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    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.

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


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Palonosetron HCl
    Br J Pharmacol. 1995 Feb; 114(4): 851–859.
     
    Palonosetron HCl
    Br J Pharmacol. 1995 Feb; 114(4): 851–859.
     
    Palonosetron HCl
    Br J Pharmacol. 1995 Feb; 114(4): 851–859.


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