Fluphenazine (dihydrochloride) [146-56-5]

Katalog-Nummer HY-A0081-100mg

Size : 100mg

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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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Fluphenazine dihydrochloride Chemische Struktur

Fluphenazine dihydrochloride Chemische Struktur

CAS. Nr. : 146-56-5

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of Fluphenazine dihydrochloride:

  • Fluphenazine-d8 dihydrochloride In-stock
  • Fluphenazine decanoate In-stock
  • Fluphenazine Angebot einholen
  • Fluphenazine dimaleate Angebot einholen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

Beschreibung

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[1][2][3][4][6].

In Vivo

Fluphenazine (1 mg/kg; IG, treated from day 6 to day 15 of gestation) dihydrochloride causes malformations in pregnant mice[5].
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.

Klinische Studie
Molekulargewicht

510.44

Formel

C22H28Cl2F3N3OS

CAS. Nr.

146-56-5

Unlabeled CAS

Appearance

Solid

Color

White to off-white

SMILES

OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(C(F)(F)F)C=C24)CC1.10Cl.10Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9591 mL 9.7955 mL 19.5909 mL
5 mM 0.3918 mL 1.9591 mL 3.9182 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 (stored under nitrogen). 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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: ≥ 2.08 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.
  • Protocol 2

    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.

  • Protocol 1

    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:

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Reinheit & Dokumentation

Purity: 99.89%

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]

  • [1]. Zhou X, et al. The neuroleptic drug, fluphenazine, blocks neuronal voltage-gated sodium channels. Brain Res. 2006;1106(1):72-81.

    [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.

    [3]. Siragusa S, Bistas KG, Saadabadi A. Fluphenazine. 2022 May 8. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan.

    [4]. Davis JL, et al. Peripheral diabetic neuropathy treated with amitriptyline and fluphenazine. JAMA. 1977 Nov 21;238(21):2291-2.

    [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.

    [6]. Langwiński R, Niedzielski J. Narcotic analgesics and stereotyped behaviour in mice. Naunyn Schmiedebergs Arch Pharmacol. 1980 Jul;312(3):225-7.

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). 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.

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Fluphenazine dihydrochloride Related Classifications

Help & FAQs

Keywords:

Fluphenazine146-56-5Dopamine ReceptorSARS-CoVSodium ChannelSARS coronavirusNa channelsNa+ channelsneuronal voltage-gated sodium channelsoralschizophreniaphenothiazinegnawingclimbing behaviourpsychosisdiabetesSARS-CoV-2malformationsSwiss-Webster miceInhibitorinhibitorinhibit

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