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  3. Pirinixic acid

Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

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CAS No. : 50892-23-4

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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of Pirinixic acid:

Top Publications Citing Use of Products

33 Publications Citing Use of MCE Pirinixic acid

IF
RT-PCR
2D/3D Cell Culture and Differentiation
IHC

    Pirinixic acid purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 29:e17049.  [Abstract]

    RT-qPCR analysis of FADS2 and indicated genes in HaCaT cells pretreated with 50 μM WY14643 or DMSO for 21 h, followed by PBS or M5 stimulation for 3 h.

    Pirinixic acid purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9.  [Abstract]

    Crypts isolated from Lgr5-EGFP-IRES-creERT2 mice were cultured with CA together with/without 100 μM WY14643/ 10 μM Pioglitazone/ 1 μM GW501516 for 6 days. Representative staining pattern of Lgr5+ cells.

    Pirinixic acid purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9.  [Abstract]

    Crypts isolated from Lgr5-EGFP-IRES-creERT2 mice were cultured with 50 μM CA together with/without 100 μM WY14643 for 6 days. The mRNA level of a specified gene.

    Pirinixic acid purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9.  [Abstract]

    Crypts isolated from Lgr5-EGFP-IRES-creERT2 mice were cultured with 50 μM CA together with/without 100 μM for 6 days. Representative images analysis of organoid budding.

    Pirinixic acid purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9.  [Abstract]

    WY14643 (1 mg/kg; i.g.). Colitic WT mice were administered with vehicle or WY14643. Representative H&E staining images of intestinal segments.

    View All PPAR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

    IC50 & Target[1]

    PPARα

    0.63 μM (EC50)

    PPARγ

    32 μM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    COS-7 EC50
    39.8 μM
    Compound: 1, WY-14,643
    Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
    Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
    [PMID: 25022880]
    COS-7 EC50
    53.7 μM
    Compound: 1
    Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
    Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
    [PMID: 20307981]
    COS-7 EC50
    53.7 μM
    Compound: 1, WY-14,643
    Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
    Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
    [PMID: 25022880]
    COS-7 IC50
    36.3 μM
    Compound: 1
    Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
    Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
    [PMID: 25037914]
    COS-7 IC50
    53.7 μM
    Compound: 1
    Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
    Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
    [PMID: 25037914]
    CV-1 EC50
    0.13 μM
    Compound: Wy14643
    Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 22579420]
    HEK293 EC50
    23.33 μM
    Compound: WY-14643
    Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
    [PMID: 23265844]
    HepG2 EC50
    0.04 μM
    Compound: WY-14643
    Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
    Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
    [PMID: 19053776]
    HepG2 EC50
    1.56 μM
    Compound: Wy 14,643
    Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
    Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
    [PMID: 23171045]
    HepG2 EC50
    1.56 μM
    Compound: Wy-14,643
    Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay
    Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay
    [PMID: 25462281]
    HepG2 EC50
    1.6 μM
    Compound: WY-14643
    Effective concentration against human PPARalpha expressed in HepG2 cells
    Effective concentration against human PPARalpha expressed in HepG2 cells
    [PMID: 16107150]
    HepG2 EC50
    1.6 μM
    Compound: WY-14643
    Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
    Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
    [PMID: 18835719]
    HepG2 EC50
    1.6 μM
    Compound: WY-14643
    Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
    Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
    [PMID: 19775169]
    HepG2 EC50
    1.6 μM
    Compound: WY-14643
    Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
    Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
    [PMID: 22081932]
    HepG2 EC50
    1.6 μM
    Compound: Wy-14,643
    Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
    Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
    [PMID: 22341573]
    HepG2 EC50
    1.62 μM
    Compound: WY-14643
    Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
    Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
    [PMID: 19053776]
    HepG2 EC50
    1.62 μM
    Compound: Wy-14,643
    Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
    Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
    [PMID: 25497132]
    HepG2 EC50
    3.46 μM
    Compound: WY14643
    Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay
    Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay
    [PMID: 23502212]
    HepG2 EC50
    4.8 μM
    Compound: WY-14643
    Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
    Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
    [PMID: 18625559]
    HepG2 EC50
    4800 nM
    Compound: WY-14643
    Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
    Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
    [PMID: 21450468]
    HepG2 EC50
    7.1 μM
    Compound: WY14643
    Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
    Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
    [PMID: 23502212]
    MCF7 EC50
    542 nM
    Compound: WY-14643
    Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay
    Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay
    [PMID: 24936232]
    MCF7 EC50
    650 nM
    Compound: WY-14643
    Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
    Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
    [PMID: 24936232]
    U2OS EC50
    12 μM
    Compound: WY-14643
    Agonist activity at human PPARalpha in U2OS cells by transactivation assay
    Agonist activity at human PPARalpha in U2OS cells by transactivation assay
    [PMID: 18329751]
    U2OS EC50
    20 μM
    Compound: WY-14643
    Effect on PPARalpha transactivation activity in U2OS cells
    Effect on PPARalpha transactivation activity in U2OS cells
    [PMID: 16300944]
    In Vitro

    Pirinixic acid (Wy-14643) is an agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively[1].
    Pirinixic acid (Wy-14643; 0, 10, 100 μM) enhances protein expression of PPAR-α in synovial fibroblasts. Pirinixic acid (0, 10, 100 μM) shows inhibitroy effects on NO and PGE2 production in LPS-stimulated synovial fibroblasts. Pirinixic acid also effectively downregulates expression of inflammatory mediators such as VCAM-1, ICAM-1, ET-1, and TF in synovial fibroblasts, blocks LPS-induced NF-kB activation, IkB phosphorylation, and NF-kB nuclear translocation in synovial fibroblasts, but Pirinixic acid shows no effects in PPAR-α silenced cells[2].

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

    In Vivo

    Pirinixic acid (Wy-14643; 10 mg/kg, i.v.) decreases hepatic injury and lipid peroxidation (MDA) levels in obese rats. Pirinixic acid also causes increased SIRT1 activity in Sham and ischemia-reperfusion (IR) group, but shows no effects on SIRT3 protein expression. Pirinixic acid enhances NAD+, and ATP levels, and prevents endoplasmic reticulum stress (ERS) in rats[3].

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

    Molecular Weight

    323.80

    Formula

    C14H14ClN3O2S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CSC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (308.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0883 mL 15.4416 mL 30.8833 mL
    5 mM 0.6177 mL 3.0883 mL 6.1767 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: 10 mg/mL (30.88 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 10 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 (100.0 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: ≥ 2.08 mg/mL (6.42 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.
    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:
    %
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    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: 99.34%

    References
    Cell Assay
    [2]

    Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Pirinixic acid. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Pirinixic acid. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve[2].

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

    Animal Administration
    [2]

    Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Wy-14643. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Wy-14643. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve[2].

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

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0883 mL 15.4416 mL 30.8833 mL 77.2082 mL
    5 mM 0.6177 mL 3.0883 mL 6.1767 mL 15.4416 mL
    10 mM 0.3088 mL 1.5442 mL 3.0883 mL 7.7208 mL
    15 mM 0.2059 mL 1.0294 mL 2.0589 mL 5.1472 mL
    20 mM 0.1544 mL 0.7721 mL 1.5442 mL 3.8604 mL
    25 mM 0.1235 mL 0.6177 mL 1.2353 mL 3.0883 mL
    30 mM 0.1029 mL 0.5147 mL 1.0294 mL 2.5736 mL
    40 mM 0.0772 mL 0.3860 mL 0.7721 mL 1.9302 mL
    50 mM 0.0618 mL 0.3088 mL 0.6177 mL 1.5442 mL
    60 mM 0.0515 mL 0.2574 mL 0.5147 mL 1.2868 mL
    80 mM 0.0386 mL 0.1930 mL 0.3860 mL 0.9651 mL
    100 mM 0.0309 mL 0.1544 mL 0.3088 mL 0.7721 mL
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      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.

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    Product Name:
    Pirinixic acid
    Cat. No.:
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