Palonosetron hydrochloride

Pricing Availability   Qty
Description: Highly potent and high affinity 5-HT3 antagonist
Chemical Name: (3aS)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one hydrochloride
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for Palonosetron hydrochloride

Palonosetron hydrochloride is a highly potent and high affinity 5-HT3 antagonist (IC50 = 0.24 nM for 5-HT3A; pKi = 10.4). Displays a slow dissociation rate. Inhibits 5-HT-induced enhancement of cellular response to substance P (Cat. No. 1156) in vitro. Inhibits cisplatin (Cat. No. 2251)-induced enhancement of substance P response in vivo.

Technical Data for Palonosetron hydrochloride

M. Wt 332.87
Formula C19H24N2O.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 135729-62-3
PubChem ID 6918303
Smiles O=C1N([C@@H]2CN3CCC2CC3)C[C@@]4([H])CCCC5=C4C1=CC=C5.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Palonosetron hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 33.29 100
DMSO 3.33 10

Preparing Stock Solutions for Palonosetron hydrochloride

The following data is based on the product molecular weight 332.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3 mL 15.02 mL 30.04 mL
5 mM 0.6 mL 3 mL 6.01 mL
10 mM 0.3 mL 1.5 mL 3 mL
50 mM 0.06 mL 0.3 mL 0.6 mL

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Product Datasheets for Palonosetron hydrochloride

References for Palonosetron hydrochloride

References are publications that support the biological activity of the product.

Wong et al (1995) The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br.J.Pharmacol. 114 851 PMID: 7773546

Rojas et al (2010) The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivo. J.Pharmacol.Exp.Ther. 335 362 PMID: 20724484

Lummis & Thompson (2013) Agonists and antagonists induce different palonosetron dissociation rates in 5-HT3A and 5-HT3AB receptors. Neuropharmacology. 73 241 PMID: 23747573

Del Cadia et al (2013) Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor. Bioorg.Med.Chem. 21 7523 PMID: 24128813

If you know of a relevant reference for Palonosetron hydrochloride, please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

5-HT Receptors Scientific Review

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.