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Paliperidone Palmitate {[allProObj[0].p_purity_real_show]}

货号：A967105

Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester prodrug of Paliperidone. Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.

Paliperidone Palmitate 化学结构
CAS号：199739-10-1

Paliperidone Palmitate 3D分子结构
CAS号：199739-10-1

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Paliperidone Palmitate 纯度/质量文件产品仅供科研

货号：A967105 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

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多巴胺受体亚型比较
5-羟色胺受体亚型比较

产品名称	D1 receptor ↓ ↑	D2 receptor ↓ ↑	D3 receptor ↓ ↑	D4 receptor ↓ ↑	D5 receptor ↓ ↑	DAT ↓ ↑	Dopamine receptor ↓ ↑	其他靶点	纯度
Penfluridol	+ Dopamine receptor, Ki: 1.6 μM								98%
Ansofaxine HCl	++ Dopamine receptor, IC50: 491 nM								98%
Tetrahydroberberine,THB		+ D2 receptor, pKi: 6.08							98+%
Prochlorperazine Maleate		✔							95%
Olanzapine		✔							99+%
Trifluoperazine		++++ Dopamine D2 receptor, IC50: 1.1 nM							98%
Ropinirole hydrochloride		++ D2 receptor, Ki: 29 nM							99%
Lurasidone		++++ D2 receptor, Ki: 1 nM							98%
Levosulpiride		✔							99+%
Pridopidine		✔							95%
Metoclopramide		✔					✔		99+%
Molindone HCl		✔							98%
Sulpiride		✔							99+%
Perospirone		++++ D2 receptor, Ki: 1.4 nM							99%
Perospirone HCl		++++ D2 receptor, Ki: 1.4 nM							98+%
Phenothiazine		✔							98%
Pimozide	+ Dopamine D1 receptor, Ki: 6600 nM	+++ Dopamine D2 receptor, Ki: 3.0 nM	++++ Dopamine D3 receptor, Ki: 0.83 nM						98%
Rotundine	++ D1 receptor, IC50: 166 nM	+ D2 receptor, IC50: 1.47 μM	+ D3 receptor, IC50: 3.25 μM						98%
Domperidone		✔							99+%
ONC206		✔							97%
Pimethixene maleate	++ Dopamine D1 Receptor, pKi: 6.37	+++ Dopamine D2 Receptor, pKi: 8.19		++ Dopamine D4.4 Receptor, pKi: 7.54					97%
Loxapine succinate	++ D1 receptor (human), Ki: 26 nM D2 receptor (Human), Ki: 62 nM	++ D2 receptor (bovine), Ki: 26 nM D2 receptor (human), Ki: 24 nM		+++ D4 receptor (human), Ki: 7.5 nM					99%
Chlorprothixene	+++ D1 receptor, Ki: 18 nM	+++ D2 receptor, Ki: 2.96 nM	+++ D3 receptor, Ki: 4.56 nM		+++ D5 receptor, Ki: 9 nM				98%
SCH-23390 HCl	++++ D1 dopamine receptor, Ki: 0.2 nM				++++ D5 dopamine receptor, Ki: 0.3 nM				98%
MPP+ iodide						✔			97%
σ1 Receptor antagonist-1						+ DAT, pKi: 5.8			97%
Benztropine mesylate						++ DAT, IC50: 118 nM			98%
Azaperone							✔		98%
Ziprasidone HCl							✔		98+%
Paliperidone							✔		98%
Alizapride HCl							✔		99+%
Amisulpride							✔		98%
Quetiapine hemifumarate							✔	Adrenergic Receptor	98%
Clozapine N-oxide							✔		99%
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。

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	✔								98%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								98%
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	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	98%
Fluoxetine HCl	✔								99.5%
Paroxetine hydrochloride	✔							AChR	97%
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						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						98% HPLC
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						99%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
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-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
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-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 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-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
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。

Paliperidone Palmitate 生物活性

描述

Paliperidone is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against^[2]. The drug proved to be efficacious in both acute psychotic symptoms treatment and long-term treatment. Its efficacy in patients with schizophrenia was similar and sometimes even better than the efficacy of other long-acting drugs, such as risperidone or olanzapine^[3]. Once-monthly injectable paliperidone palmitate (PDP) has demonstrated comparable efficacy as 1st-generation long-acting injectable antipsychotics (LAIAs) in reducing disease severity and re-hospitalizations in schizophrenic patients. However, PDP leads to significantly less extrapyramidal symptoms than these older medications indicating a superior safety profile^[4].

Paliperidone Palmitate 参考文献

[1]Kwon JS, et al. Satisfaction of immediate or delayed switch to paliperidone palmitate in patients unsatisfied with current oral atypical antipsychotics. Int Clin Psychopharmacol. 2015;30(6):320-328.

[2]Kwon JS, Kim SN, Han J, Lee SI, Chang JS, Choi JS, Lee HJ, Cho SJ, Jun TY, Lee SH, Han C, Lee KU, Lee KK, Lee E. Satisfaction of immediate or delayed switch to paliperidone palmitate in patients unsatisfied with current oral atypical antipsychotics. Int Clin Psychopharmacol. 2015 Nov;30(6):320-8

[3]Jarema M, Bieńkowski P, Heitzman J, Parnowski T, Rybakowski J. Paliperidone palmitate: effectiveness, safety, and the use for treatment of schizophrenia. Psychiatr Pol. 2017 Feb 26;51(1):7-21. English, Polish

[4]Morris MT, Tarpada SP. Long-Acting Injectable Paliperidone Palmitate: A Review of Efficacy and Safety. Psychopharmacol Bull. 2017 May 15;47(2):42-52

Paliperidone Palmitate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.50mL

0.30mL

0.15mL

7.52mL

1.50mL

0.75mL

15.04mL

3.01mL

1.50mL

Paliperidone Palmitate 技术信息

CAS号	199739-10-1
分子式	C₃₉H₅₇FN₄O₄
分子量	664.893

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

无水乙醇: 2 mg/mL(3.01 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验配方

Paliperidone Palmitate {[allProObj[0].p_purity_real_show]}

Paliperidone Palmitate 纯度/质量文件产品仅供科研

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Paliperidone Palmitate {[allProObj[0].p_purity_real_show]}

Paliperidone Palmitate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Paliperidone Palmitate 质控信息

Paliperidone Palmitate 生物活性

Paliperidone Palmitate 参考文献

Paliperidone Palmitate 实验方案

Paliperidone Palmitate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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