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Palonosetron

Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

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  • 10mg
    ¥2437.00
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  • 货号: ajce57930
  • CAS: 135729-61-2
  • 别名: 帕洛诺司琼
  • 分子式: C19H24N2O
  • 分子量: 296.41
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).


Palonosetron is a 5-HT3 receptor antagonist with a high binding affinity for this receptor and little or no affinity for other receptors[1].


Palonosetron has a longer half-life and a higher binding affinity than the first-generation 5-HT3 receptor antagonists. After intravenous dosing of palonosetron in healthy subjects and cancer patients, an initial decline in plasma concentration is followed by a slow elimination from the body. Mean maximum plasma concentration and area under the concentration-time curves are generally dose-proportional over the dose range of 0.3 to 90 μg/kg in healthy subjects and in cancer patients. Palonosetron has a volume of distribution of approximately 8.3 ± 2.5 L/kg and is 62% bound to plasma proteins. It is eliminated from the body through renal excretion and metabolic pathways. The mean terminal elimination half-life is approximately 40 hours[1].


[1] Rudolph M Navari. Cancer Manag Res. 2009, 1: 167-176. [2] Price KL, et al. ACS Chem Neurosci. 2016, 7(12):1641-1646.

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