Perphenazine (Synonyms: 奋乃静)

目录号: HY-A0077 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Perphenazine 是一种具有口服活性的多巴胺受体 (dopamine receptor) 和组胺-1 受体 (histamine-1 receptor) 拮抗剂, K_i 值分别为 0.56 nM (D2)、0.43 nM (D3)、0.6 nM (5-HT2A)。Perphenazine 还可与 Alpha-1A 肾上腺素受体 (Alpha-1A adrenergic receptor) 结合。Perphenazine 抑制癌细胞增殖，并诱导细胞凋亡。Perphenazine 可用于精神疾病、癌症、炎症的研究。

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Perphenazine Chemical Structure

CAS No. : 58-39-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
500 mg	￥500	In-stock
1 g	￥600	In-stock
5 g	￥1300	In-stock
10 g		询价
50 g		询价

or 大包装询价

* Please select Quantity before adding items.

Other Forms of Perphenazine:

MCE 顾客使用本产品发表的 1 篇科研文献

•Toxicol Lett. 29 July 2022.

Perphenazine 相关产品

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

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

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α adrenergic receptor β adrenergic receptor

生物活性
纯度 & 产品资料
参考文献

生物活性

Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation^[1]^[3]^[5].

IC₅₀ & Target^[1]

D₂ Receptor

0.56 nM (Ki)

D₃ Receptor

0.43 nM (Ki)

D₄ Receptor

28.5 nM (Ki)

5-HT_2A Receptor

5.6 nM (Ki)

5-HT₆ Receptor

17 nM (Ki)

5-HT₇ Receptor

23 nM (Ki)

H₂ Receptor

132 nM (Ki)

5-HT_1A Receptor

421 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
AN3-CA	IC₅₀	25.4 μM Compound: PPZ	Antiproliferative activity against human AN3CA cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human AN3CA cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
CHO-K1	IC₅₀	0.3 nM Compound: Perphenazine	Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay	[PMID: 23675993]
FL5.12	IC₅₀	4.8 μM Compound: 4	Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis	[PMID: 31383588]
HEC-1-A	IC₅₀	23.3 μM Compound: PPZ	Antiproliferative activity against human Hec1A cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human Hec1A cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
HEC-1B cell line	IC₅₀	29.8 μM Compound: PPZ	Antiproliferative activity against human HEC1B cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human HEC1B cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
HUVEC	IC₅₀	97.76 μM Compound: Perphenazine	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
Ishikawa	IC₅₀	19.4 μM Compound: PPZ	Antiproliferative activity against human Ishikawa cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human Ishikawa cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
KLE	IC₅₀	30.8 μM Compound: PPZ	Antiproliferative activity against human KLE cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human KLE cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
L02	IC₅₀	> 160 μM Compound: SYSU-20611S	Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	10.1039/C3MD00397C
MCF7	IC₅₀	35.81 μM Compound: Perphenazine	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	30.37 μM Compound: Perphenazine	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	31.77 μM Compound: Perphenazine	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]

体外研究
(In Vitro)

Perphenazine (40 μM, 48 h) inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells^[2].
Perphenazine (30 μM, 24 h) induces intense lysosome vacuolation, impaired lysosomal membrane, and induces lysosomal membrane permeabilization (LMP), ultimately triggering lysosomal cell death in L02 cells^[2].
Perphenazine (10-40 μM, 24 h) inhibits autophagic flux in L02 cells^[2].
Perphenazine (1 µM, 24 h) decreases glioblastoma U-87 MG cell migration and invasion^[4].

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

Cell Viability Assay^[2]

Cell Line:	L02 cells
Concentration:	10-100 μM
Incubation Time:	12, 24, 48 h
Result:	Inhibited cell viability in a concentration and time-dependent manner.

Western Blot Analysis^[2]

Cell Line:	L02 cells
Concentration:	10, 20, 30, and 40 μM
Incubation Time:	24 h
Result:	Increased LC3 I/II and P62/SQSTM1 levels

Cell Migration Assay ^[4]

Cell Line:	U-87 MG cells
Concentration:	1 µM
Incubation Time:	0, 3, 6, 9, 12, and 24 h
Result:	Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%.

体内研究
(In Vivo)

Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) induces liver injury and lysosomal membrane damage in ICR mice^[2].
Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis^[3].

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

Animal Model:	ICR mice^[2]
Dosage:	10, 30, 60, 120, 180 mg/kg
Administration:	Oral gavage, every other day for 21 days.
Result:	Increased histological injury and aminotransferases compared with control.

Animal Model:	Oxazolone-treated animal model of dermatitis^[3]
Dosage:	10 mg/kg
Administration:	Oral administration, every other day for 6 days
Result:	Decreased The levels of mice ear swelling.

Clinical Trial

分子量

403.97

Formula

C₂₁H₂₆ClN₃OS

CAS 号

58-39-9

性状

固体

颜色

White to off-white

中文名称

奋乃静；过非那嗪；羟哌氯丙嗪；丕芬那辛

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (247.54 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4754 mL	12.3772 mL	24.7543 mL
5 mM	0.4951 mL	2.4754 mL	4.9509 mL
10 mM	0.2475 mL	1.2377 mL	2.4754 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.19 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.19 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.19 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (635 KB) SDS (393 KB)

COA (285 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Richtand NM, et al. Dopamine and serotonin receptor binding and antipsychotic efficacy. Neuropsychopharmacology. 2007 Aug;32(8):1715-26. [Content Brief]

[2]. Lei Tao, et al. Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo. Toxicol Lett. 2022 Jul 29;367:76-87. [Content Brief]

[3]. Min-Jeong Heo, et al. Perphenazine Attenuates the Pro-Inflammatory Responses in Mouse Models of Th2-Type Allergic Dermatitis. Int J Mol Sci. 2020 May 3;21(9):3241. [Content Brief]

[4]. Michał Otręba, et al. Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, α-tubulin and integrins (α3, α5, and β1) levels. Oncol Lett. 2022 Jun;23(6):182. [Content Brief]

[5]. Michał Otręba, et al. n vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review. J Appl Toxicol. 2021 Jan;41(1):82-94. [Content Brief]

Perphenazine 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4754 mL	12.3772 mL	24.7543 mL	61.8858 mL
	5 mM	0.4951 mL	2.4754 mL	4.9509 mL	12.3772 mL
	10 mM	0.2475 mL	1.2377 mL	2.4754 mL	6.1886 mL
	15 mM	0.1650 mL	0.8251 mL	1.6503 mL	4.1257 mL
	20 mM	0.1238 mL	0.6189 mL	1.2377 mL	3.0943 mL
	25 mM	0.0990 mL	0.4951 mL	0.9902 mL	2.4754 mL
	30 mM	0.0825 mL	0.4126 mL	0.8251 mL	2.0629 mL
	40 mM	0.0619 mL	0.3094 mL	0.6189 mL	1.5471 mL
	50 mM	0.0495 mL	0.2475 mL	0.4951 mL	1.2377 mL
	60 mM	0.0413 mL	0.2063 mL	0.4126 mL	1.0314 mL
	80 mM	0.0309 mL	0.1547 mL	0.3094 mL	0.7736 mL
	100 mM	0.0248 mL	0.1238 mL	0.2475 mL	0.6189 mL

Help & FAQs

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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.

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Perphenazine (Synonyms: 奋乃静)

Other Forms of Perphenazine:

MCE 顾客使用本产品发表的 1 篇科研文献

Perphenazine 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Dopamine Receptor 亚型特异性产品:

查看 Histamine Receptor 亚型特异性产品:

查看 5-HT Receptor 亚型特异性产品:

查看 Adrenergic Receptor 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Perphenazine 相关分类

完整储备液配制表

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Perphenazine (Synonyms: 奋乃静)

Other Forms of Perphenazine:

Perphenazine 相关抗体

MCE 顾客使用本产品发表的 1 篇科研文献

Perphenazine 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Dopamine Receptor 亚型特异性产品:

查看 Histamine Receptor 亚型特异性产品:

查看 5-HT Receptor 亚型特异性产品:

查看 Adrenergic Receptor 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Perphenazine 相关抗体:

摩尔计算器

稀释计算器

Perphenazine 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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