Penfluridol (Synonyms: R-16341)

Name: Penfluridol
Brand: MedChemExpress
SKU: HY-B1077
Rating: 5.0 (7 reviews)

Cat. No.: HY-B1077 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

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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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Penfluridol Chemical Structure

CAS No. : 26864-56-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 27	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 27	In-stock	Estimated Time of Arrival: December 31
Solid
25 mg	USD 25	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 45	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
1 g	USD 245	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Penfluridol:

Penfluridol (Standard) Get quote

7 Publications Citing Use of MCE Penfluridol

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[2]

D₂ 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	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
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

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.

Molecular Weight

523.97

Formula

C₂₈H₂₇ClF₅NO

CAS No.

26864-56-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
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: 2.5 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.
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.
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:

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Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (282 KB) SDS (419 KB)

COA (246 KB) LCMS (89 KB) Elemental Analysis Report (104 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

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Penfluridol (Synonyms: R-16341)

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Other Forms of Penfluridol:

7 Publications Citing Use of MCE Penfluridol

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Penfluridol (Synonyms: R-16341)

Customer Review

Other Forms of Penfluridol:

Penfluridol Related Antibodies

7 Publications Citing Use of MCE Penfluridol

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