| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
Perphenazine:https://utheses.univie.ac.at/detail/53792
"]| Targets |
Perphenazine diHCl targets multiple receptors including dopamine receptors (D2, D3, D4), serotonin receptors (5-HT2A, 5-HT6, 5-HT7, 5-HT2C, 5-HT1A), histamine-1 receptor, and Alpha-1A adrenergic receptor. It acts as an antagonist with Ki values of 0.56 nM (D2), 0.43 nM (D3), 5.6 nM (5-HT2A), 17 nM (5-HT6), 23 nM (5-HT7), 28.5 nM (D4), 132 nM (5-HT2C), and 421 nM (5-HT1A). It also binds to Alpha-1A adrenergic receptor and histamine-1 receptor.
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| ln Vitro |
In L02 cells, 40 μM perphenazine dihydrochloride promotes apoptosis mediated by CTSD (Cathepsin D) and reduces cell viability[2]. When perphenazine (30 μM, 24 h) dihydrochloride is added to L02 cells, it causes lysosomal cell death by causing severe vacuolation of the lysosome, defective lysosomal membrane, and lysosomal membrane permeabilization (LMP)[2]. In L02 cells, autophagic flow is inhibited by perphenazine (10–40 μM, 24 h) dihydrochloride[2]. Perphenazine (1 µM, 24 h) dihydrochloride inhibits the migration and invasion of glioblastoma U-87 MG cells[4].
In vitro, Perphenazine diHCl (40 μM, 48 h) inhibits cell viability and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells. At 30 μM for 24 h, it induces intense lysosome vacuolation, impaired lysosomal membrane, and lysosomal membrane permeabilization (LMP), ultimately triggering lysosomal cell death in L02 cells. It inhibits autophagic flux in L02 cells at 10-40 μM for 24 h. At 1 μM for 24 h, it decreases glioblastoma U-87 MG cell migration and invasion. Cell viability is inhibited in a concentration and time-dependent manner (10-100 μM, 12-48 h). |
| ln Vivo |
In ICR mice, perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) dihydrochloride causes damage to the liver and lysosomal membranes[2]. In mouse models of Th2-type allergic dermatitis, perphenazine (oral administration, 10 mg/kg, every other day for 6 days) dihydrochloride attenuates morphological phenotype[3].
In vivo, Perphenazine diHCl administered by oral gavage at 180 mg/kg every other day for 21 days induces liver injury and lysosomal membrane damage in ICR mice. At 10 mg/kg oral administration every other day for 6 days, it attenuates morphological phenotype. In ICR mice, doses of 10, 30, 60, 120, and 180 mg/kg by oral gavage every other day for 21 days increased histological injury and aminotransferases compared with control. |
| Enzyme Assay |
In vitro receptor binding assays are performed using radioligand competition binding to determine Ki values for dopamine, serotonin, histamine, and adrenergic receptors. Membrane preparations from cells expressing the target receptors are incubated with radiolabeled ligands and varying concentrations of Perphenazine diHCl. Bound radioactivity is measured by scintillation counting, and Ki values are calculated from competition curves using the Cheng-Prusoff equation.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: L02 cells Tested Concentrations: 10-100 μM Incubation Duration: 12, 24, 48 h Experimental Results: Inhibited cell viability in a concentration and time -dependent manner. Western Blot Analysis[2] Cell Types: L02 cells Tested Concentrations: 10, 20, 30, and 40 μM Incubation Duration: 24 h Experimental Results: Increased LC3 I/II and P62/SQSTM1 levels Cell Migration Assay [4] Cell Types: U-87 MG cells Tested Concentrations: 0, 3, 6, 9, 12, and 24 h Incubation Duration: 0, 3, 6, 9, 12, and 24 h Experimental Results: Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%. In vitro cell-based assays are conducted in L02 cells and U-87 MG glioblastoma cells. For cell viability assays, cells are treated with Perphenazine diHCl at 10-100 μM for 12, 24, or 48 h, and viability is measured by MTT or similar assays. For apoptosis assays, cells are treated at 40 μM for 48 h and apoptosis markers including CTSD-mediated pathways are assessed. For migration assays, U-87 MG cells are treated with 1 μM for 24 h and wound closure is measured. Western blot analysis for LC3 I/II and p62/SQSTM1 is performed at 10-40 μM for 24 h to assess autophagic flux. |
| Animal Protocol |
Animal/Disease Models: ICR mice[2]
Doses: 10, 30, 60, 120, 180 mg/kg Route of Administration: po (oral gavage), every other day for 21 days. Experimental Results: Increased histological injury and aminotransferases compared with control. Animal/Disease Models: Oxazolone-treated animal model of dermatitis[3] Doses: 10 mg/kg Route of Administration: Oral administration, every other day for 6 days Experimental Results: diminished The levels of mice ear swelling . In vivo animal experiments are conducted in ICR mice. Perphenazine diHCl is administered by oral gavage at doses of 10, 30, 60, 120, and 180 mg/kg every other day for 21 days. Liver injury is assessed by measuring serum aminotransferases and histological examination of liver tissue. Lysosomal membrane damage is evaluated by appropriate staining and imaging techniques. The compound is formulated as a suspension in appropriate vehicle for oral administration. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Perphenazine diHCl include oral activity and good oral bioavailability. The compound is absorbed after oral administration and distributes to target tissues including the brain. As a phenothiazine antipsychotic, it undergoes hepatic metabolism primarily via cytochrome P450 enzymes. Specific PK parameters such as half-life, Cmax, and AUC have not been extensively detailed in the available literature. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
In vivo toxicology studies in ICR mice demonstrate that Perphenazine diHCl at oral doses of 180 mg/kg every other day for 21 days induces liver injury and lysosomal membrane damage. Increased histological injury and elevated aminotransferases are observed at doses of 10-180 mg/kg. In vitro, the compound induces lysosomal cell death through lysosomal membrane permeabilization. Comprehensive toxicology data are limited; the compound is for research use only and not for human therapeutic use.
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| References |
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| Additional Infomation |
Perphenazine diHCl (CAS: 2015-28-3) has molecular formula C21H28Cl3N3OS and molecular weight 476.89. Synonyms: Trilafon, Etaperazine, Perphenazin, Perfenazine, Chlorpiprazine. It is a first-generation antipsychotic belonging to the piperazinyl phenothiazine class. Purity: ≥98%. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Not approved for clinical use; for research purposes only. The compound is used for studying psychiatric disorders, cancer, and inflammation.
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| Molecular Formula |
C21H26N3OSCL.2[HCL]
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|---|---|
| Molecular Weight |
476.89052
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| Exact Mass |
475.102
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| CAS # |
2015-28-3
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| Related CAS # |
Perphenazine;58-39-9;Perphenazine-d8 dihydrochloride;2070015-23-3
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| PubChem CID |
74835
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
580.4ºC at 760mmHg
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| Flash Point |
304.8ºC
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| Vapour Pressure |
2.6E-14mmHg at 25°C
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| LogP |
5.487
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
463
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)N(CCCN3CCN(CC3)CCO)C4=C(C=CC(=C4)Cl)S2.Cl.Cl
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| InChi Key |
JGTYANSBOIVAMH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26ClN3OS.2ClH/c22-17-6-7-21-19(16-17)25(18-4-1-2-5-20(18)27-21)9-3-8-23-10-12-24(13-11-23)14-15-26;;/h1-2,4-7,16,26H,3,8-15H2;2*1H
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| Chemical Name |
2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0969 mL | 10.4846 mL | 20.9692 mL | |
| 5 mM | 0.4194 mL | 2.0969 mL | 4.1938 mL | |
| 10 mM | 0.2097 mL | 1.0485 mL | 2.0969 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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