Art. -Nr.: HY-119980

Fluphenazine

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine 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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Reinheit: 98.70%
CAS. Nr.: 69-23-8
Formel: C₂₂H₂₆F₃N₃OS
Molecular Weight:437.52

Speicherung:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fluphenazine Chemical Structure

CAS. Nr.: 69-23-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Dopamine receptor, Sodium channels, SARS-CoV-2^[1]^[2]

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	110 μM Compound: fluphenazine	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	[PMID: 18788725]
HepG2	IC₅₀	4.4 μM Compound: SYSU-20913S	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	10.1039/C3MD00397C
HUVEC	IC₅₀	38.01 μM Compound: Fluphenazine	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]
L02	IC₅₀	>160 μM Compound: SYSU-20913S	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
LoVo	IC₅₀	80 μM Compound: Fluphenazine	Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 37060756]
MCF7	IC₅₀	24.57 μM Compound: Fluphenazine	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	16.73 μM Compound: Fluphenazine	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	18.56 μM Compound: Fluphenazine	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]
NIH-3T3-G185	IC₅₀	10.4 μM Compound: Fluphenazine	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	5.7 μM Compound: Fluphenazine	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	6.5 μM Compound: Fluphenazine	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]

In Vivo

Fluphenazine (1 mg/kg; IG, treated from day 6 to day 15 of gestation) causes malformations in pregnant mice^[5].
Fluphenazine (0.125-1 mg/kg; IP, single dosage) 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.

Animal Model:

Mice (injected with 60 mg/kg Methylphenidate)^[6]
Dosage:

0.125, 0.25, 0.5, and 1 mg/kg
Administration:

IP, single dosage
Result:

Antagonized Methylphenidate-induced stereotyped gnawing; inhibited significantly climbing behaviour in mice at 0.0625-0.5 mg/kg, and at the dose of 1 mg/kg abolished this effect completely.

Animal Model:

Mature female Swiss-Webster mice^[5]
Dosage:

1 mg/kg
Administration:

IG, treated from day 6 to day 15 of gestation
Result:

Significantly reduced fetal weight and length, increased the incidence of incomplete ossification of sternebrae and skull bones.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 69-23-8
Appearance Oil
Molecular Weight 437.52
Formel C₂₂H₂₆F₃N₃OS
Color Colorless to off-white
SMILES

OCCN1CCN(CC1)CCCN2C3=C(SC4=C2C=C(C=C4)C(F)(F)F)C=CC=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

Nat Commun

Gut microbiota modulates aversive learning and memory of honeybees (Apis mellifera). [Abstract]

2025 Dec 18;16(1):11196. PMID: 41413037
Dev Cell

Sestrin2 drives ER-phagy in response to protein misfolding. [Abstract]

2024 Aug 19;59(16):2035-2052.e10. PMID: 39094564
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (228.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2856 mL

11.4280 mL

22.8561 mL

5 mM

0.4571 mL

2.2856 mL

4.5712 mL

10 mM

0.2286 mL

1.1428 mL

2.2856 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 5 mg/mL (11.43 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

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

Solubility: ≥ 5 mg/mL (11.43 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (11.43 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (796 KB)
- English - EN (796 KB)
- Français - FR (796 KB)
- Deutsch - DE (796 KB)
- Norwegian - NO (796 KB)
- Español - ES (796 KB)
- Swedish - SV (796 KB)
- Italian - IT (796 KB)
- Korean - KR (796 KB)
- Portuguese - PT (796 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.2856 mL	11.4280 mL	22.8561 mL	57.1402 mL
	5 mM	0.4571 mL	2.2856 mL	4.5712 mL	11.4280 mL
	10 mM	0.2286 mL	1.1428 mL	2.2856 mL	5.7140 mL
	15 mM	0.1524 mL	0.7619 mL	1.5237 mL	3.8093 mL
	20 mM	0.1143 mL	0.5714 mL	1.1428 mL	2.8570 mL
	25 mM	0.0914 mL	0.4571 mL	0.9142 mL	2.2856 mL
	30 mM	0.0762 mL	0.3809 mL	0.7619 mL	1.9047 mL
	40 mM	0.0571 mL	0.2857 mL	0.5714 mL	1.4285 mL
	50 mM	0.0457 mL	0.2286 mL	0.4571 mL	1.1428 mL
	60 mM	0.0381 mL	0.1905 mL	0.3809 mL	0.9523 mL
	80 mM	0.0286 mL	0.1429 mL	0.2857 mL	0.7143 mL
	100 mM	0.0229 mL	0.1143 mL	0.2286 mL	0.5714 mL

Keywords

Fluphenazine

3 Cited Publications

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Fluphenazine

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Publications Citing Use of MedChemExpress (MCE) Fluphenazine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fluphenazine Related Classifications

HY-119980 Related Classifications