Fluphenazine dihydrochloride
Based on 4 publication(s) in Google Scholar
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.
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- Pureté : 99.91%
- CAS No.: 146-56-5
- Formule: C22H28Cl2F3N3OS
- Masse moléculaire:510.44
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Stockage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
110 μM
Compound: fluphenazine
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Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
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[PMID: 18788725] |
| HepG2 | IC50 |
4.4 μM
Compound: SYSU-20913S
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
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10.1039/C3MD00397C |
| HUVEC | IC50 |
38.01 μM
Compound: Fluphenazine
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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
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[PMID: 34435487] |
| L02 | IC50 |
>160 μM
Compound: SYSU-20913S
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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
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10.1039/C3MD00397C |
| MCF7 | IC50 |
24.57 μM
Compound: Fluphenazine
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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
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[PMID: 34435487] |
| MDA-MB-231 | IC50 |
16.73 μM
Compound: Fluphenazine
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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
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[PMID: 34435487] |
| MDA-MB-231 | IC50 |
18.56 μM
Compound: Fluphenazine
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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
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[PMID: 34435487] |
| Vero C1008 | CC50 |
20.02 μM
Compound: Fluphenazine Dihydrochloride
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CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
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10.1101/2020.03.25.008482 |
| Vero C1008 | CC50 |
20.02 μM
Compound: Fluphenazine Dihydrochloride
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CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
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10.1101/2020.03.25.008482 |
| Vero C1008 | IC50 |
6.36 μM
Compound: Fluphenazine Dihydrochloride
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IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
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10.1101/2020.03.25.008482 |
| Vero C1008 | IC50 |
8.98 μM
Compound: Fluphenazine Dihydrochloride
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IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
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10.1101/2020.03.25.008482 |
In Vivo
Fluphenazine (0.125-1 mg/kg; IP, single dosage) dihydrochloride antagonizes Methylphenidate-induced stereotyped gnawing; inhibits significantly climbing behaviour[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 146-56-5
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Appearance Solid
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Masse moléculaire 510.44
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Formule C22H28Cl2F3N3OS
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Color White to off-white
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SMILES
OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(C(F)(F)F)C=C24)CC1.[H]Cl.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 Dec 18;16(1):11196. PMID: 41413037 -
Dev Cell
2024 Aug 19;59(16):2035-2052.e10. PMID: 39094564
Fluphenazine dihydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Aug 19;59(16):2035-2052.e10. [Abstract]
Fluphenazine dihydrochloride (10 μM; 12 h) increased the protein expression of mKeima-RAMP4 in RCS cells.
Fluphenazine dihydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Aug 19;59(16):2035-2052.e10. [Abstract]
Fluphenazine dihydrochloride (10 μM; 12 h) increased the protein expression of TFE3 in TFEB/TFE3 DKO U2OS cells.
Fluphenazine dihydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Aug 19;59(16):2035-2052.e10. [Abstract]
Fluphenazine dihydrochloride (10 μM; 12 h) increased the RNA expression of FAM134B isoform 2 in WT and TFEB/3 DKO RCS cells.
Fluphenazine dihydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Aug 19;59(16):2035-2052.e10. [Abstract]
Fluphenazine dihydrochloride (10 μM; 12 h) reduced GFP-COL1A2 G610C protein levels in control but not in FAM134B-, TFEB/TFE3-, and ATG7-depleted cells.
Fluphenazine dihydrochloride purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Aug 19;59(16):2035-2052.e10. [Abstract]
Fluphenazine dihydrochloride (10 μM; 12 h) showed no effect on the levels of insoluble ATZ from PIZ hepatocytes.
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Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998 -
Solvant et solubilité
In Vitro:
H2O : 100 mg/mL (195.91 mM; Need ultrasonic)
DMSO : ≥ 38 mg/mL (74.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (195.91 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocole
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureté et documentation
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Fiche technique (275 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Zhou X, et al. The neuroleptic drug, fluphenazine, blocks neuronal voltage-gated sodium channels. Brain Res. 2006;1106(1):72-81. [Content Brief]
[2]. Nazeam J, et al. Based on Principles and Insights of COVID-19 Epidemiology, Genome Sequencing, and Pathogenesis: Retrospective Analysis of Sinigrin and ProlixinRX (Fluphenazine) Provides Off-Label Drug Candidates. SLAS Discov. 2020 Dec;25(10):1123-1140. [Content Brief]
[3]. Siragusa S, Bistas KG, Saadabadi A. Fluphenazine. 2022 May 8. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan. [Content Brief]
[4]. Davis JL, et al. Peripheral diabetic neuropathy treated with amitriptyline and fluphenazine. JAMA. 1977 Nov 21;238(21):2291-2. [Content Brief]
[5]. Abdel-Hamid HA, et al. Teratogenic effect of diphenylhydantoin and/or fluphenazine in mice. J Appl Toxicol. 1996 May-Jun;16(3):221-5. [Content Brief]
[6]. Langwiński R, Niedzielski J. Narcotic analgesics and stereotyped behaviour in mice. Naunyn Schmiedebergs Arch Pharmacol. 1980 Jul;312(3):225-7. [Content Brief]
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 (stored under nitrogen, away from moisture). 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 / H2O | 1 mM | 1.9591 mL | 9.7955 mL | 19.5909 mL | 48.9774 mL |
| 5 mM | 0.3918 mL | 1.9591 mL | 3.9182 mL | 9.7955 mL | |
| 10 mM | 0.1959 mL | 0.9795 mL | 1.9591 mL | 4.8977 mL | |
| 15 mM | 0.1306 mL | 0.6530 mL | 1.3061 mL | 3.2652 mL | |
| 20 mM | 0.0980 mL | 0.4898 mL | 0.9795 mL | 2.4489 mL | |
| 25 mM | 0.0784 mL | 0.3918 mL | 0.7836 mL | 1.9591 mL | |
| 30 mM | 0.0653 mL | 0.3265 mL | 0.6530 mL | 1.6326 mL | |
| 40 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2244 mL | |
| 50 mM | 0.0392 mL | 0.1959 mL | 0.3918 mL | 0.9795 mL | |
| 60 mM | 0.0327 mL | 0.1633 mL | 0.3265 mL | 0.8163 mL | |
| H2O | 80 mM | 0.0245 mL | 0.1224 mL | 0.2449 mL | 0.6122 mL |
| 100 mM | 0.0196 mL | 0.0980 mL | 0.1959 mL | 0.4898 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Fluphenazine dihydrochloride Related Classifications
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