Cat. No.: HY-B1077

Penfluridol

(Synonyms: R-16341)

9 Cited Publications

Avis client

Based on 9 publication(s) in Google Scholar

Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 μg/ml.

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Pureté: 99.84%
CAS No.: 26864-56-2
Formule: C₂₈H₂₇ClF₅NO
Masse moléculaire:523.97

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Penfluridol Chemical Structure

CAS No.: 26864-56-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[2]

D₂ Receptor

Voir tous les produits spécifiques à Isoform Calcium Channel :

Voir tous les produits spécifiques à Isoform Dopamine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
H4	EC₅₀	3.2 μM Compound: 2	Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis Induction of autophagy in human H4 cells expressing LC3 using DAPI staining after 4 hrs by fluorescence microscopic analysis	[PMID: 21126871]
Lewis lung carcinoma cell line	IC₅₀	4.2 μM Compound: PFL	Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30389290]
Lewis lung carcinoma cell line	IC₅₀	4.3 μM Compound: PFL	Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30389290]
Lewis lung carcinoma cell line	IC₅₀	6 μM Compound: PFL	Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against mouse LLC cells harboring luciferin assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30389290]
MDA-MB-231	IC₅₀	2.3 μM Compound: 1	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33039722]
MDA-MB-231	IC₅₀	5 μM Compound: PFL	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30389290]
MDA-MB-231	IC₅₀	5.1 μM Compound: PFL	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30389290]
MDA-MB-231	IC₅₀	6.1 μM Compound: PFL	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30389290]
NIH3T3	IC₅₀	6.01 μM Compound: PFL	Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30389290]
NIH3T3	IC₅₀	6.03 μM Compound: PFL	Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 30389290]
NIH3T3	IC₅₀	6.09 μM Compound: PFL	Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30389290]
Vero	CC₅₀	8.77 μM Compound: Penfluridol	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	5.01 μM Compound: Penfluridol	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Penfluridol (R-16341; 1.25-40 μM; 24, 48 h) reduces cell viability of human AML cells harboring FLT3-WT or the FLT3-ITD mutation^[2].
Penfluridol (7.5 μM; 24 h) results in the apoptosis of AML cells harboring FLT3-WT and FLT3-ITD mutation^[2].
Penfluridol (1.25-7.5 μM; 24 h) induces ROS-mediated autophagy via triggering LC3 turnover and acidic vesicular organelle (AVO) formation^[2].
Penfluridol (1 μM; for 2 h) obviously inhibits TNFα-induced phosphorylation levels of ERK, JNK, and p38^[3].
Penfluridol (1 μM; for 2 h) inhibits TNFα-induced mRNA expressions of IL-1β, IL-6, IL-17, and NOS2^[3].
Penfluridol suppresses the differentiation of spleen naive CD4+T cells to TH1 and TH17 and inhibits M1 macrophage polarization^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:

Human AML cell lines, HL-60 (FLT3-WT), U937 (FLT3-WT), and MV4–11 (FLT3-ITD)
Concentration:

1.25, 2.5, 5, 10, 20, 40 μM
Incubation Time:

24, 48 h
Result:

Significantly reduced cell viability in a concentration-dependent manner.

Apoptosis Analysis^[2]

Cell Line:

HL-60 and U937 cells harboring FLT3-WT
Concentration:

7.5 μM
Incubation Time:

24 h
Result:

Induced concentration-dependent increases in the sub-G1 population.
Triggered caspase-3 activation and corresponding PARP-1 cleavage in concentration- and time-dependent manners.

Cell Autophagy Assay^[2]

Cell Line:

U937 and HL-60 cells
Concentration:

1.25, 2.5, 5, 7.5 μM
Incubation Time:

24 h
Result:

5 μM and 7.5 μM respectively induced dominant LC3B-II formation and caspase-3 activation in U937 and HL-60 cells.

Western Blot Analysis^[3]

Cell Line:

BMDMs
Concentration:

1 μM
Incubation Time:

Pretream for 2 h
Result:

Obviously inhibited the increased phosphorylation levels of ERK, JNK, and p38 by TNFα (10 ng/mL; 15, 30, 60 min).

RT-PCR^[3]

Cell Line:

BMDMs
Concentration:

1 μM
Incubation Time:

Pretream for 2 h
Result:

Inhibited TNFα-induced mRNA expressions of IL-1β, IL-6, IL-17, and NOS2.

In Vivo

Penfluridol (10 mg/kg; daily oral gavage; from the 18th day after the first immunization) significantly reduced severity of collagen-induced arthritis^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

DBA/1J male mice aged 10–12 weeks with type II chicken collagen-induced arthritis (CIA) model^[3]
Dosage:

10 mg/kg
Administration:

Daily oral gavage; from the 18th day after the first immunization
Result:

Inhibited inflammatory cell infiltration, suppressed pannus formation, and protected articular cartilage from damage.
obviously decreased mRNA expressions of CXCL10 and MCP-1 in inflamed joints and statistically reduced production levels of inflammatory cytokines IL-1β and IL-6 in sera.

Essai clinique

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

Chemical Information

CAS No. 26864-56-2
Appearance Solid
Masse moléculaire 523.97
Formule C₂₈H₂₇ClF₅NO
Color White to off-white
SMILES

OC1(C2=CC=C(Cl)C(C(F)(F)F)=C2)CCN(CCCC(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC1
Synonyms

R-16341
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (9)

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Journal Impact Factor

Cell Commun Signal

Inhibition of AMPK/PFKFB3 mediated glycolysis synergizes with penfluridol to suppress gallbladder cancer growth. [Abstract]

2022 Jul 16;20(1):105. PMID: 35842652

Penfluridol purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2022 Jul 16;20(1):105. [Abstract]

The cell viability measured by the CCK-8 assay of SGC-996, EH-GB1, and GBC-SD cells were treated with Penfluridol (PF, 0-10 μM) as indicated for 24 h/48 h.

Penfluridol purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2022 Jul 16;20(1):105. [Abstract]

The colony formation of SGC-996, EH-GB1, and GBC-SD cells were seeded in 6-well plates and treated with Penfluridol (PF, 0-2 μM) as indicated for 14 days.

Penfluridol purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2022 Jul 16;20(1):105. [Abstract]

Annexin V/PI staining apoptosis assay of SGC-996, EH-GB1, and GBC-SD cells treated with Penfluridol (PF, 0-7.5 μM) as indicated for 24 h.

Penfluridol purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2022 Jul 16;20(1):105. [Abstract]

The Western blotting of SGC-996, EH-GB1, and GBC-SD were treated with Penfluridol (PF, 0-7.5 μM) as indicated for 24 h.

Penfluridol purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2022 Jul 16;20(1):105. [Abstract]

Cell cycle assay of SGC-996, EH-GB1, and GBC-SD cells treated with Penfluridol (PF, 0-7.5 μM) as indicated for 24 h.
Biomed Pharmacother

Penfluridol regulates p62 / Keap1 / Nrf2 signaling pathway to induce ferroptosis in osteosarcoma cells. [Abstract]

2024 Jul 11:177:117094. PMID: 38996707
Int Immunopharmacol

Dysregulated neutrophils contribute to bone loss in renal osteodystrophy by enhancing osteoclastogenesis: Insights from integrated bioinformatics and experimental validation. [Abstract]

2026 Jan 1;168(Pt 2):115947. PMID: 41314047
Arthritis Res Ther

Penfluridol targets acid sphingomyelinase to inhibit TNF signaling and is therapeutic against inflammatory autoimmune diseases. [Abstract]

2022 Jan 19;24(1):27. PMID: 35045889
Microbiologyopen

Drug repurposing: Antimicrobial and antibiofilm effects of penfluridol against Enterococcus faecalis. [Abstract]

2021 Jan;10(1):e1148. PMID: 33345466
Mediators Inflamm

Penfluroidol Attenuates the Imbalance of the Inflammatory Response by Repressing the Activation of the NLRP3 Inflammasome and Reduces Oxidative Stress via the Nrf2/HO-1 Signaling Pathway in LPS-Induced Macrophages. [Abstract]

2023 Aug 22:2023:9940858. PMID: 37650025
Sci Rep

Penfluridol synergizes with colistin to reverse colistin resistance in Gram-negative bacilli. [Abstract]

2025 May 8;15(1):16114. PMID: 40341530
J Ocul Pharmacol Ther

Survey of Dopamine Receptor D2 Antagonists as Retinal Antifibrotics. [Abstract]

2024 Oct;40(8):536-542. PMID: 39206555
Research Square Preprint

2021 Dec.

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (190.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.9085 mL

9.5425 mL

19.0851 mL

5 mM

0.3817 mL

1.9085 mL

3.8170 mL

10 mM

0.1909 mL

0.9543 mL

1.9085 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.77 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (479 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[1]. Eyal Zur, et al. Penfluridol, a Unique Psychiatric Medicine for the Treatment of Chronic Schizophrenia. Int J Pharm Compd. 2019 Mar-Apr;23(2):113-119. [Content Brief]

[2]. Szu-Yuan Wu, et al. Penfluridol triggers cytoprotective autophagy and cellular apoptosis through ROS induction and activation of the PP2A-modulated MAPK pathway in acute myeloid leukemia with different FLT3 statuses. J Biomed Sci. 2019 Aug 31;26(1):63. [Content Brief]

[3]. Yue-Hong Chen, et al. Penfluridol targets acid sphingomyelinase to inhibit TNF signaling and is therapeutic against inflammatory autoimmune diseases. Arthritis Res Ther. 2022 Jan 19;24(1):27. [Content Brief]

[4]. Xianghai Zeng, et al. Drug repurposing: Antimicrobial and antibiofilm effects of penfluridol against Enterococcus faecalis. Microbiologyopen. 2021 Jan;10(1):e1148. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9085 mL	9.5425 mL	19.0851 mL	47.7127 mL
	5 mM	0.3817 mL	1.9085 mL	3.8170 mL	9.5425 mL
	10 mM	0.1909 mL	0.9543 mL	1.9085 mL	4.7713 mL
	15 mM	0.1272 mL	0.6362 mL	1.2723 mL	3.1808 mL
	20 mM	0.0954 mL	0.4771 mL	0.9543 mL	2.3856 mL
	25 mM	0.0763 mL	0.3817 mL	0.7634 mL	1.9085 mL
	30 mM	0.0636 mL	0.3181 mL	0.6362 mL	1.5904 mL
	40 mM	0.0477 mL	0.2386 mL	0.4771 mL	1.1928 mL
	50 mM	0.0382 mL	0.1909 mL	0.3817 mL	0.9543 mL
	60 mM	0.0318 mL	0.1590 mL	0.3181 mL	0.7952 mL
	80 mM	0.0239 mL	0.1193 mL	0.2386 mL	0.5964 mL
	100 mM	0.0191 mL	0.0954 mL	0.1909 mL	0.4771 mL

Penfluridol

9 Cited Publications

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Penfluridol

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Publications Citing Use of MedChemExpress (MCE) Penfluridol

Voir tous les produits spécifiques à Isoform Calcium Channel

Voir tous les produits spécifiques à Isoform Dopamine Receptor

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Penfluridol Related Classifications

HY-B1077 Related Classifications