| Size | Price | Stock | Qty |
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| 10mg |
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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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Purity: ≥98%
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. In order to avoid acute and delayed nausea and vomiting that are linked to both initial and repeated courses of highly emetogenic cancer chemotherapy, the FDA approved the use of fosnetupitant and palonosetron in April of 2018. With a ± hundred-fold higher 5-HT3 receptor binding affinity than other 5-HT3 receptor antagonists (pKi 10.5 compared with 8.91 for granisetron, 8.81 for tropisetron, 8.39 for ondansetron, and 7.6 for dolasetron), palonosetron is a highly potent, selective, second-generation antagonist of the 5-HT3 receptor pathway.
| Targets |
5-HT3 Receptor
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| ln Vitro |
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| ln Vivo |
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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 |
C19H25CLN2O3
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|---|---|
| Molecular Weight |
332.87
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| Exact Mass |
332.17
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| Elemental Analysis |
C, 68.56; H, 7.57; Cl, 10.65; N, 8.42; O, 4.81
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| CAS # |
135729-62-3
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| Related CAS # |
Palonosetron-d3 hydrochloride; 1246816-81-8; Palonosetron; 135729-61-2; (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.Cl
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| InChi Key |
OLDRWYVIKMSFFB-SSPJITILSA-N
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| InChi Code |
InChI=1S/C19H24N2O.ClH/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;1H/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;hydrochloride
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| Synonyms |
RS-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; 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) |
Solubility in Formulation 1: ≥ 0.33 mg/mL (0.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.33 mg/mL (0.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 3.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.33 mg/mL (0.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (300.42 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0042 mL | 15.0209 mL | 30.0418 mL | |
| 5 mM | 0.6008 mL | 3.0042 mL | 6.0084 mL | |
| 10 mM | 0.3004 mL | 1.5021 mL | 3.0042 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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