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 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.

For research use only. We do not sell to patients.

Perphenazine Chemical Structure

Perphenazine Chemical Structure

CAS No. : 58-39-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Perphenazine:

Perphenazine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Perphenazine

View All Dopamine Receptor Isoform Specific Products:

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

View All Histamine Receptor Isoform Specific Products:

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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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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]
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].

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

Perphenazine Related Antibodies

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%.
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].

MedChemExpress (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
Molecular Weight

403.97

Formula

C21H26ClN3OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(Cl)C=C24)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (247.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

SDS (393 KB)

COA (247 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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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Perphenazine Related Classifications

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:

Perphenazine58-39-9Dopamine ReceptorHistamine Receptor5-HT ReceptorAdrenergic ReceptorApoptosisAutophagySerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorMental diseaseliver injuryhepatotoxicitydermatitisinflammationU-87 MG cellsanti-cancerlysosomeInhibitorinhibitorinhibit

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