Palonosetron hydrochloride | Palonosetron (hydrochloride);RS 25259;RS 25259 197;Palonosetron HCl | 帕洛诺司琼盐酸盐 | 5-HT Receptor

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Palonosetron HCl/盐酸帕洛诺司琼 {[allProObj[0].p_purity_real_show]}

货号：A195751 同义名： 帕洛诺司琼盐酸盐 / Palonosetron (hydrochloride); RS 25259

Palonosetron HCl 是一种卡宾唑派生物，选择性 5-HT3 受体拮抗剂。

Palonosetron HCl/盐酸帕洛诺司琼化学结构
CAS号：135729-62-3

Palonosetron HCl/盐酸帕洛诺司琼 3D分子结构
CAS号：135729-62-3

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Palonosetron HCl/盐酸帕洛诺司琼纯度/质量文件产品仅供科研

货号：A195751 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Nat. Electron., 2025, 8, 66-74. Ambeed. [ A100095 ]; • Nano-Micro Lett., 2025, 17, 311. Ambeed. [ A971305 ]; • Adv. Mater., 2025, 2416621. Ambeed. [ A255324 , A420052 ]; • Adv. Mater., 2025, 2410493. Ambeed. [ A838608 ]; 更多 >

5-羟色胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM								98%
Venlafaxine	✔								99%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								97%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	99%
Fluoxetine HCl	✔								99.5%
Paroxetine HCl	✔							AChR	99%
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						95%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						99%
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM						99%+
Loxapine succinate			++ 5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						98%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	99%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron HCl dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron HCl				++++ 5-HT3, IC50: 0.33 nM					99%
Asenapine maleate		+++ 5-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		97%
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2B, pKi: 6.2 5-HT2A, pKi: 6.6			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Palonosetron HCl/盐酸帕洛诺司琼生物活性

描述

Palonosetron hydrochloride, as 5-HT3 receptor antagonist palonosetron, is an important treatment for emesis and nausea during cancer therapy. Chronic exposure to palonosetron reduced the number of available cell surface [3H]granisetron binding sites^[3]. Combining low-dose palonosetron with droperidol potentiated prophylaxis for PONV (Postoperative nausea and vomiting) and achieved a similar prophylactic effect^[4]. Moreover, palonosetron significantly adds to the clinician’s ability to effectively control CINV (chemotherapy-induced nausea and vomiting) in patients undergoing HEC or MEC (highly and moderately emetogenic chemotherapy)^[5].

Palonosetron HCl/盐酸帕洛诺司琼参考文献

[1]Gralla R, Lichinitser M, et al. Palonosetron improves prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy: results of a double-blind randomized phase III trial comparing single doses of palonosetron with ondansetron. Ann Oncol. 2003 Oct;14(10):1570-7.

[2]Wong EH, Clark R, et al. The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br J Pharmacol. 1995 Feb;114(4):851-9.

[3]Hothersall JD, Moffat C, Connolly CN. Prolonged inhibition of 5-HT₃ receptors by palonosetron results from surface receptor inhibition rather than inducing receptor internalization. Br J Pharmacol. 2013 Jul;169(6):1252-62.

[4]Hu X, Tan F, Gong L. Higher dose of palonosetron versus lower dose of palonosetron plus droperidol to prevent postoperative nausea and vomiting after eye enucleation and orbital hydroxyapatite implant surgery: a randomized, double-blind trial. Drug Des Devel Ther. 2017 May 15;11:1465-1472.

[5]Celio L, Niger M, Ricchini F, Agustoni F. Palonosetron in the prevention of chemotherapy-induced nausea and vomiting: an evidence-based review of safety, efficacy, and place in therapy. Core Evid. 2015 Aug 21;10:75-87.

Palonosetron HCl/盐酸帕洛诺司琼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

15.02mL

3.00mL

1.50mL

30.04mL

6.01mL

3.00mL

Palonosetron HCl/盐酸帕洛诺司琼技术信息

CAS号	135729-62-3
分子式	C₁₉H₂₅ClN₂O
分子量	332.87
SMILES Code	O=C1N([C@@H]2CN3CCC2CC3)C[C@]4([H])C5=C1C=CC=C5CCC4.[H]Cl
MDL No.	MFCD07370072

别名	帕洛诺司琼盐酸盐 ;Palonosetron (hydrochloride); RS 25259; RS 25259 197; Palonosetron HCl
运输	蓝冰
InChI Key	OLDRWYVIKMSFFB-SSPJITILSA-N
Pubchem ID	6918303

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 3 mg/mL(9.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 100 mg/mL(300.42 mM)，配合低频超声助溶

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Palonosetron HCl/盐酸帕洛诺司琼纯度/质量文件产品仅供科研

Palonosetron HCl/盐酸帕洛诺司琼质控信息

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Palonosetron HCl/盐酸帕洛诺司琼实验方案

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