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

Perphenazine 

Cat. No.: HY-A0077 Purity: 99.95%
COA Handling Instructions

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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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Perphenazine

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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)

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.

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)

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
10 mM 0.2475 mL 1.2377 mL 2.4754 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.95%

References
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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.

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Perphenazine
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HY-A0077
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