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  2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis Autophagy
  3. Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy
  4. Perphenazine

Perphenazine  (Synonyms: 奮乃靜)

目錄號(hào): HY-A0077 純度: 99.95%
COA 產(chǎn)品使用指南

Perphenazine 是一種具有口服活性的多巴胺受體 (dopamine receptor) 和組胺-1 受體 (histamine-1 receptor) 拮抗劑, Ki 值分別為 0.56 nM (D2)、0.43 nM (D3)、0.6 nM (5-HT2A)。Perphenazine 還可與 Alpha-1A 腎上腺素受體 (Alpha-1A adrenergic receptor) 結(jié)合。Perphenazine 抑制癌細(xì)胞增殖，并誘導(dǎo)細(xì)胞凋亡。Perphenazine 可用于精神疾病、癌癥、炎癥的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Perphenazine Chemical Structure

Perphenazine Chemical Structure

CAS No. : 58-39-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
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   詢價(jià)  
50 g   詢價(jià)  

* Please select Quantity before adding items.

Other Forms of Perphenazine:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki 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-HT2A Receptor

5.6 nM (Ki)

5-HT6 Receptor

17 nM (Ki)

5-HT7 Receptor

23 nM (Ki)

H2 Receptor

132 nM (Ki)

5-HT1A Receptor

421 nM (Ki)

細(xì)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]
體外研究
(In Vitro)

Perphenazine (40 μM，48 h) 抑制細(xì)胞活力，并誘導(dǎo) L02 細(xì)胞中由 CTSD (Cathepsin D) 介導(dǎo)的細(xì)胞凋亡[2]。
Perphenazine (30 μM，24 h) 誘導(dǎo)細(xì)胞凋亡強(qiáng)烈的溶酶體空泡形成，破壞溶酶體膜，并誘導(dǎo)溶酶體膜透化 (LMP)，最終引發(fā) L02 細(xì)胞中的溶酶體細(xì)胞死亡[2]。
Perphenazine (10-40 μM，24 h) 抑制 L02 細(xì)胞中的自噬流[2]。
Perphenazine (1 μM，24 小時(shí)) 減少膠質(zhì)母細(xì)胞瘤 U-87 MG 細(xì)胞遷移和侵襲[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%.
體內(nèi)研究
(In Vivo)

奮乃靜 (口服灌胃，180 mg/kg，隔日給藥，連續(xù) 21 天) 誘導(dǎo) ICR 小鼠肝損傷和溶酶體膜損傷[2]。
奮乃靜 (口服，10 mg/kg) kg，每隔一天，持續(xù) 6 天) 減弱 Th2 型過(guò)敏性皮炎小鼠模型的形態(tài)學(xué)表型[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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

奮乃靜；過(guò)非那嗪；羥哌氯丙嗪；丕芬那辛
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (247.54 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.19 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.19 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
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產(chǎn)品名稱：
Perphenazine
目錄號(hào)：
HY-A0077
需求量：