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  3. PPAR
  4. Pemafibrate

Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.

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

CAS No. : 848259-27-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Pemafibrate:

Pemafibrate Related Antibodies

Top Publications Citing Use of Products

    Pemafibrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2021 Apr;37(2):293-311.  [Abstract]

    a ATP content in NASH-triggered hSKP-HPC upon increasing concentrations of PPAR agonists (Pemafibrate; 60, 100, 200 μM; 24 h). b ATP content in NASH-triggered HepG2, HepaRG and PHH cultures upon exposure to PPAR agonists at a concentration of 60 µM.

    Pemafibrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2021 Apr;37(2):293-311.  [Abstract]

    Pemafibrate (60 μM) reduces lipid levels only in HepG2 and PHH. Micrographs of in vitro NASH models stained for neutral lipids with BODIPY™ 493/503 (green) and DAPI (blue, nuclei).

    Pemafibrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2021 Apr;37(2):293-311.  [Abstract]

    Pemafibrate (10 μM) decreased the ACTA2 and COL1A1 mRNA level, increased the LOXL2 mRNA levels in human LX-2 stellate cells.

    Pemafibrate purchased from MedChemExpress. Usage Cited in: Open Biol. 2019 Dec;9(12):190141.  [Abstract]

    Pemafibrate increased the protein expression of CCL2 in stable CCL2 knockdown HUVECs.

    Pemafibrate purchased from MedChemExpress. Usage Cited in: Open Biol. 2019 Dec;9(12):190141.  [Abstract]

    Pemafibrate did not inhibit HUVEC apoptosis when CCL2 expression was inhibited.

    View All PPAR Isoform Specific Products:

    View All Isoforms
    PPARα PPARβ/δ PPARγ PPAR PPARδ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.

    IC50 & Target[1]

    h-PPARα

    1 nM (EC50)

    h-PPARγ

    1.1 μM (EC50)

    PPARδ

    1.58 μM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    HEK-293T EC50
    1 nM
    Compound: SC-3
    Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay
    Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay
    		[PMID: 25491112]
    In Vitro

    Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively. Pemafibrate is more than 1000 fold selective towards PPARα than PPARγ and PPARδ[1].

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

    Pemafibrate Related Antibodies
    In Vivo

    Pemafibrate (3 mg/kg, p.o.) increases plasma h-apoA-I in human apoA-I (h-apoA-I) transgenic mice, and shows higher levels of plasma h-apoA-I than fenofibrate at 300 mg/kg[1]. Pemafibrate (0.03 mg/kg) decreases levels of triglycerides and aspartate aminotransferase (AST) in PEMA-L (db/db) mice. Pemafibrate (0.1 mg/kg) not only shows such effects but increases liver weight in PEMA-H (db/db) mice. Pemafibrate enhances the pathogenesis in a rodent model of nonalcoholic steatohepatitis (NASH). Pemafibrate significantlly reduces the grade of hepatocyte ballooning in PEMA-H mice. Furthermore, Pemafibrate modulates lipid turnover and induces uncoupling protein 3 (UCP 3) expression in the liver[2]. Pemafibrate (K-877, 0.0005%) contained in high-fat diet (HFD) inhibits the body weight gain in mice. Pemafibrate significantly decreases the abundance of triglyceride (TG)-rich lipoproteins, including remnants, in postprandial plasma of mice. Pemafibrate also decreases intestinal mRNA expression of ApoB and Npc1l1[3].

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

    490.55

    Formula

    C28H30N2O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC[C@@H](OC1=CC=CC(CN(C2=NC3=CC=CC=C3O2)CCCOC4=CC=C(OC)C=C4)=C1)C(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (203.85 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 2.0385 mL 10.1926 mL 20.3853 mL
    5 mM 0.4077 mL 2.0385 mL 4.0771 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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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

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    C2

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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: ≥ 2.5 mg/mL (5.10 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 (5.10 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: 99.85%

    SDS (393 KB)

    COA (246 KB) HNMR (260 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [2]

    Mice are fasted for 12 h and fasting blood glucose measured. Nine-week-old db/db mice are used in the assay. After a 2-week acclimatization period, mice are divided into four groups: BD (db/db) mice (fed basal diet (BD) and treated with 0.5% aqueous methylcellulose solution (MC); MCD (db/db) mice (fed methionine choline-deficient (MCD) and treated with 0.5% MC); PEMA-L (db/db) mice (fed MCD and treated with 0.03 mg/kg Pemafibrate); PEMA-H (db/db) mice (fed MCD and treated with 0.1 mg/kg Pemafibrate). The drug-free solvent or the dosing solution is administered to animals (5 mL/kg body weight, p.o.) once daily (in the morning) for 4 consecutive weeks. After a 2-week acclimatization period, BD mice are fed a BD for 20 weeks. CTRL mice are fed D09100301 for 20 weeks. PEMA-L and PEMA-H mice are fed D09100301 for 12 weeks followed by D09100301 with 0.4 mg and 1.3 mg Pemafibrate/kg of the diet for 8 weeks, which corresponds to 0.03 mg/kg/day and 0.1 mg/kg/day, respectively. FENO mice are fed D09100301 for 12 weeks followed by D09100301 with 666.7 mg fenofibrate/kg of the diet for 8 weeks, which corresponds to 50 mg/kg/day. Pemafibrate and fenofibrate are incorporated into the AMLN diet. Animals are housed under conventional conditions with controlled temperature, humidity, and light (12-h light-dark cycle) and provided with food and water[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, 6 months; -20°C, 1 month. 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 1 mM 2.0385 mL 10.1926 mL 20.3853 mL 50.9632 mL
    5 mM 0.4077 mL 2.0385 mL 4.0771 mL 10.1926 mL
    10 mM 0.2039 mL 1.0193 mL 2.0385 mL 5.0963 mL
    15 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3975 mL
    20 mM 0.1019 mL 0.5096 mL 1.0193 mL 2.5482 mL
    25 mM 0.0815 mL 0.4077 mL 0.8154 mL 2.0385 mL
    30 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
    40 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2741 mL
    50 mM 0.0408 mL 0.2039 mL 0.4077 mL 1.0193 mL
    60 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
    80 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
    100 mM 0.0204 mL 0.1019 mL 0.2039 mL 0.5096 mL
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    Pemafibrate 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:

    Pemafibrate848259-27-8(R)-K-13675PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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