Palonosetron

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Palonosetron is a 5-HT3 antagonist primarily used to prevent acute, delayed, and overall chemotherapy-induced nausea and vomiting. Palonosetron exhibits moderate anti-flavivirus activity and potent anti-Zika virus activity in mammalian cells. Palonosetron also possesses antidepressant activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Palonosetron hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Palonosetron Chemical Structure

CAS No. : 135729-61-2

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Other In-stock Forms of Palonosetron:

Palonosetron hydrochloride

Other Forms of Palonosetron:

Palonosetron hydrochloride In-stock
(R,R)-Palonosetron Hydrochloride Get quote

1 Publications Citing Use of MCE Palonosetron

•PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]

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•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT₃ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.83 nM Compound: Palonosetron, Aloxi	Antagonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay Antagonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay	[PMID: 24128813]
HEK293	IC₅₀	0.88 nM Compound: Palonosetron, Aloxi	Antagonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay Antagonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay	[PMID: 24128813]

In Vitro

Palonosetron (10 nM, 2 hours) inhibits the enhancement effect of 5-HT on substance P (SP)-induced calcium release in NG108-15 cells, increasing the EC₅₀ of SP from 0.62 µM to 3.7 µM^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Palonosetron (0.05 mg/kg, i.p., single dose) significantly reduces immobility in Swiss albino mice, demonstrating potential antidepressant activity^[5].
alonosetron (30-300 µg/kg, i.v., single dose) dose-dependently inhibits SP-mediated neuronal responses in the Cisplatin (HY-17394)-induced rat emesis model, indicating its impact on neurotransmission^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Swiss albino mice (25-40 g)^[5]
Dosage:	0.025 and 0.05 mg/kg
Administration:	Intraperitoneal injection (i.p.), single dose, efficacy tested after 1 hour and 24 hours
Result:	Reduced immobility time in a dose-dependent manner. The 0.05 mg/kg dose significantly reduced immobility time after 1 hour and 24 hours.

Animal Model:	Cisplatin-induced emesis model in adult male Sprague-Dawley rats (270-350 g)^[6]
Dosage:	30 µg/kg, 100 µg/kg, 300 µg/kg
Administration:	Intravenous injection (i.v.), single dose
Result:	Dose-dependently inhibited the Cisplatin (HY-17394)-induced enhancement of neuronal response to substance P (SP) in the nodose ganglia.

Clinical Trial

Molecular Weight

296.41

Formula

C₁₉H₂₄N₂O

CAS No.

135729-61-2

SMILES

O=C1N(C[C@@]([H])(CCC2)C3=C2C=CC=C13)[C@@H]4CN5CCC4CC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Barrows, et al. "A screen of FDA-approved drugs for inhibitors of Zika virus infection." Cell host & microbe 20.2 (2016): 259-270. [Content Brief]

[2]. Rojas, et al. "Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor." Anesthesia & Analgesia 107.2 (2008): 469-478. [Content Brief]

[3]. Wallenborn, et al. "Palonosetron hydrochloride in the prevention and treatment of postoperative nausea and vomiting." Clinical Medicine Insights: Therapeutics 2 (2010): CMT-S4016.

[4]. Sepúlveda-Vildósola, et al. "Palonosetron hydrochloride is an effective and safe option to prevent chemotherapy-induced nausea and vomiting in children." Archives of medical research 39.6 (2008): 601-606. [Content Brief]

[5]. Sharma J, et al. Evaluation of antidepressant effect of palonosetron in Swiss albino mice[J]. National Journal of Pharmacology and Therapeutics, 2023, 1(2): 98-100.

[6]. Rojas C, et al. The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivo. J Pharmacol Exp Ther. 2010 Nov;335(2):362-8. [Content Brief]

Palonosetron Related Classifications

Neurological Disease Infection Cardiovascular Disease

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Palonosetron135729-61-25-HT ReceptorFlavivirusSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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