2. GPCR/G Protein Neuronal Signaling Anti-infection
  3. 5-HT Receptor Flavivirus
  4. Palonosetron

Palonosetron  (Synonyms: 帕洛诺司琼)

目录号: HY-A0018
产品使用指南 技术支持

Palonosetron 是一种 5-HT3 拮抗剂，主要用于预防急性、延迟性及整体化疗引起的恶心和呕吐。此外，Palonosetron 在哺乳动物细胞中表现出中等的抗黄病毒活性和高效的抗寨卡病毒活性。Palonosetron 也具有抗抑郁活性。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Palonosetron hydrochloride 通常具有更好的水溶性和稳定性。

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Palonosetron

Palonosetron Chemical Structure

CAS No. : 135729-61-2

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Palonosetron 的其他形式现货产品:

Other Forms of Palonosetron:

Palonosetron 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 5-HT Receptor 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3][4].

IC50 & Target

5-HT3 Receptor

 

细胞效力
(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]
体外研究
(In Vitro)

Palonosetron (10 nM，2 小时) 在 NG108-15 细胞中抑制 5-HT 对 P 物质 (SP) 诱导钙释放的增强作用，将 SP 的 EC50 从 0.62 µM 提高到 3.7 µM[6]。

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

Palonosetron 相关抗体:
体内研究
(In Vivo)

Palonosetron (0.05 mg/kg，腹腔注射，单次给药) 在瑞士白化小鼠中显著减少不动时间，具有潜在抗抑郁活性[5]。
Palonosetron (30-300 µg/kg，静脉注射，单次给药) 在顺铂 (HY-17394) 诱导的大鼠呕吐模型中以剂量依赖方式抑制 SP 介导的神经反应，显示其对神经传递的影响[6]。

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
分子量

296.41

Formula

C19H24N2O
CAS 号
中文名称

帕洛诺司琼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Palonosetron 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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:

Palonosetron135729-61-2帕洛诺司琼5-HT ReceptorFlavivirusSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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