| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Palonosetron (formerly RS-25259, RS-25259 197; trade name: Aloxi and Akynzeo) is a 5-HT3 antagonist approved for use in the prevention and treatment of chemotherapy-induced nausea and vomiting. As of April 2018, the combination of fosnetupitant and palonosetron was 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).
| Targets |
5-HT3 Receptor ( Ki = 0.17 nM )
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| ln Vitro |
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| ln Vivo |
Palonosetron surpasses the first-generation 5-HT3 receptor antagonists in both half-life and binding affinity. When palonosetron is given intravenously to both healthy individuals and cancer patients, the body gradually eliminates the drug after an initial drop in plasma concentration. Between 0.3 and 90 μg/kg, the mean maximum plasma concentration and the area under the concentration-time curves in both healthy individuals and cancer patients are typically dose-proportional. With a volume of distribution of 8.3 ± 2.5 L/kg, palonosetron is 62% bound to plasma proteins. Through metabolic processes and renal excretion, it is removed from the body. 40 hours is roughly the mean terminal elimination half-life[1].
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| Enzyme Assay |
Palonosetron is a second-generation, highly selective, potent antagonist of the 5-HT3 receptor with a binding affinity for the receptor that is approximately 100 times higher than that of other antagonists of the 5-HT3 receptor (pKi 10.5 compared with 8.91 for granisetron, 8.81 for tropisetron, 8.39 for ondansetron, and 7.6 for dolasetron).
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| Cell Assay |
Palonosetron is a 5-HT3 antagonist used to treat and prevent nausea and vomiting brought on by chemotherapy (CINV). IC50 Value: Among the 5-HT3 antagonists, 5-HT3 Receptor Palonosetron is the most successful in managing delayed CINV nausea and vomiting that manifests over a 24-hour period following the initial dosage of a chemotherapy regimen.
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| Animal Protocol |
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| References |
| Molecular Formula |
C19H24N2O
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| Molecular Weight |
296.41
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| Exact Mass |
296.19
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| Elemental Analysis |
C, 76.99; H, 8.16; N, 9.45; O, 5.40
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| CAS # |
135729-61-2
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| Related CAS # |
Palonosetron hydrochloride; 135729-62-3; (R,R)-Palonosetron Hydrochloride; 135729-75-8
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| Appearance |
Solid powder
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| SMILES |
C1C[C@@H]2CN(C(=O)C3=CC=CC(=C23)C1)[C@@H]4CN5CCC4CC5
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| InChi Key |
CPZBLNMUGSZIPR-NVXWUHKLSA-N
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| InChi Code |
InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1
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| Chemical Name |
(3aS)-2-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3a,4,5,6-tetrahydro-3H-benzo[de]isoquinolin-1-one
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| Synonyms |
RS 25259; RS 25259 197; RS 25233-197; RS25233-197; RS-25233-197; RS25233-198; RS-25233-198; RS 25233-198; RS-25259-197; Palonosetron; US brand name: Aloxi; Akynzeo
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3737 mL | 16.8685 mL | 33.7371 mL | |
| 5 mM | 0.6747 mL | 3.3737 mL | 6.7474 mL | |
| 10 mM | 0.3374 mL | 1.6869 mL | 3.3737 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05956899 | Recruiting | Drug: Palonosetron Drug: Ondansetron |
Idiopathic Scoliosis Postoperative Nausea and Vomiting |
University of Malaya | June 1, 2023 | Phase 4 |
| NCT04507711 | Recruiting | Drug: 0 ul of palonosetron Drug: 1 ul of palonosetron |
Blood Coagulation Disorder | Seoul National University Bundang Hospital |
September 16, 2020 | Not Applicable |
| NCT03817970 | Recruiting | Drug: Granisetron Drug: Palonosetron |
Nephrotoxicity | University of Colorado, Denver | November 15, 2019 | Phase 3 |
| NCT05199818 | Recruiting | Drug: Palonosetron HCl Buccal Film 0.5 mg Drug: IV Palonosetron 0.25 mg |
Chemotherapy-induced Nausea and Vomiting |
Xiamen LP Pharmaceutical Co., Ltd |
March 1, 2022 | Phase 3 |
| NCT05841849 | Not yet recruiting | Drug: Aprepitant Drug: Palonosetron |
Breast Cancer Chemotherapy-induced Nausea and Vomiting |
Second Affiliated Hospital, School of Medicine, Zhejiang University |
July 2023 | Phase 4 |
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