2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Autophagy Apoptosis
  3. Calcium Channel Dopamine Receptor Autophagy Apoptosis
  4. Penfluridol

Penfluridol  (Synonyms: R-16341)

Cat. No.: HY-B1077 Purity: 99.84%
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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.

For research use only. We do not sell to patients.

Penfluridol Chemical Structure

Penfluridol Chemical Structure

CAS No. : 26864-56-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Penfluridol:

Penfluridol Related Antibodies

Top Publications Citing Use of Products

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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

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

IC50 & Target[2]

D2 Receptor

 

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.

Penfluridol Related Antibodies

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 2.5 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.
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.
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%

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

Handling Instructions (2659 KB)
References

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.

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
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Penfluridol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Penfluridol26864-56-2R-16341R16341R 16341Calcium ChannelDopamine ReceptorAutophagyApoptosisCa2+ channelsCa channelsOraldiphenylbutylpiperidineantipsychoticD2TNFαNF-κBarthritiscolitisspleen naive CD4+TTH1TH17M1 macrophagechronic schizophreniaacute psychosisTourette syndromeautoimmuneE. faecalisplanktonicInhibitorinhibitorinhibit

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