2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. PF-06424439

PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.

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

CAS No. : 1469284-78-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of PF-06424439:

PF-06424439 Related Antibodies

Top Publications Citing Use of Products

    PF-06424439 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Feb 9;44(2):383-404.e18.  [Abstract]

    Cells derived from in vivo PDX models were treated in vitro with DGAT2 inhibitor (DGAT2i, PF-06424439 methanesulfonate, 10μM) for 48 hours and cellular viability was measured by CellTiter-Glo assay.

    PF-06424439 purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Nov 30;39(22):e71249.  [Abstract]

    Lipid droplet accumulation was detected using Oil Red O staining. Oil Red O staining revealed that HILPDA overexpression boosted lipid droplet content in the cells, an effect that was attenuated by treatment with DGAT1 and DGAT2 inhibitors (PF‑06424439).

    PF-06424439 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 27;15(1):8273.  [Abstract]

    Immunofluorescence images of HAECs treated with DMSO or DGAT inhibitors (A922500, 10 µM and PF-06424439, 5 µM) for 24 h, exposed to bovine serum albumin (BSA) or OA for 12 h, and then serum-starved for 48 h (n = 20 fields from 3 independent experiments). 200 µM OA was used to stimulate LD formation. BSA was used as a control treatment. Scale bar, 20 µm.

    PF-06424439 purchased from MedChemExpress. Usage Cited in: Mol Metab. 2024 Jun:84:101953.  [Abstract]

    PF-06424439 methanesulfonate (10-20 μM; 24 or 48 h) inhibited the accumulation of lipid droplets during an induced ESC decidual process.

    PF-06424439 purchased from MedChemExpress. Usage Cited in: J Dairy Sci. 2022 Apr;105(4):3588-3600.  [Abstract]

    The effect of DGAT1 and DGAT2 inhibitor on lipid synthesis in calf primary hepatocytes. Treatments were a control group (cells cultured in RPMI-1640 basic medium for 12 h), 1.2 mM fatty acids (cells treated with 1.2 mM fatty acids for 12 h), DGAT1 inhibitor (cells treated with 0.3 μM DGAT1 inhibitor 2 for 12 h), DGAT1 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM DGAT1 inhibitor and 1.2 mM fatty acids for 12 h), DGAT2 inhibitor (cells treated with 0.3 μM PF-06424439 methanesulfonate (DGAT2 inhibitor) for 12 h), DGAT2 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM PF-06424439 methanesulfonate and 1.2 mM fatty acids for 12 h). Representative western blots of SREBF1, FASN, DGAT1, DGAT2, MTTP, and APOB.

    PF-06424439 purchased from MedChemExpress. Usage Cited in: J Dairy Sci. 2022 Apr;105(4):3588-3600.  [Abstract]

    The effect of the DGAT1 and DGAT2 inhibitors on immunofluorescence of lipid droplets in calf primary hepatocytes. Treatments were control group (cells cultured in RPMI-1640 basic medium for 12 h), 1.2 mM fatty acids (cells treated with 1.2 mM fatty acids for 12 h), DGAT1 inhibitor (cells treated with 0.3 μM DGAT1 inhibitor 2 for 12 h), DGAT1 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM DGAT1 inhibitor 2 and 1.2 mM fatty acids for 12 h), DGAT2 inhibitor (cells treated with 0.3 μM PF-06424439 methanesulfonate (DGAT2i) for 12 h), and DGAT2 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM PF-06424439 methanesulfonate and 1.2 mM fatty acids for 12 h).

    PF-06424439 purchased from MedChemExpress. Usage Cited in: J Virol. 2022 Jan 26;96(2):e0147321.  [Abstract]

    N2a cells were incubated with DGAT1 inhibitor (DGAT1i) (A922500, 10 μg/mL), DGAT2i (PF-06424439 methanesulfonate, 40 μg/mL), or a combination (A922500 plus PF-06424439 methanesulfonate) for 48 h, and cell viability was assessed by a Cell Counting kit-8 (CCK-8) assay (n = 3).

    PF-06424439 purchased from MedChemExpress. Usage Cited in: Dev Comp Immunol. 2021 Nov:124:104197.  [Abstract]

    After preincubation with 30 μM DGAT1 inhibitor or 40 μM DGAT2 inhibitor (PF-06424439) for 1 h, CIK cells were treated with 3 μM Gardiquimod for 24 h. mRNA expression of DGAT1 and DGAT2 in CIK cells.

    View All Acyltransferase Isoform Specific Products:

    View All Isoforms
    ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].

    IC50 & Target

    IC50: 14 nM (DGAT2)[1]
    In Vivo

    PF-06424439 (p.o.; 60 mg/kg/day; for 3 days) reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1].
    PF-06424439 (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].

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

    Animal Model: Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)[1]
    Dosage: 60 mg/kg
    Administration: P.o.; daily; for 3 days
    Result: Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids.
    Animal Model: Male Wistar-Han rats[1]
    Dosage: 1 mg/kg
    Administration: I.v.
    Result: Showed moderate clearance and a short half-life with t1/2=1.39 h.
    Molecular Weight

    439.94

    Formula

    C22H26ClN7O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@H]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6
    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 (227.30 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2730 mL 11.3652 mL 22.7304 mL
    5 mM 0.4546 mL 2.2730 mL 4.5461 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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 (5.68 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 (5.68 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 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
    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 2.2730 mL 11.3652 mL 22.7304 mL 56.8259 mL
    5 mM 0.4546 mL 2.2730 mL 4.5461 mL 11.3652 mL
    10 mM 0.2273 mL 1.1365 mL 2.2730 mL 5.6826 mL
    15 mM 0.1515 mL 0.7577 mL 1.5154 mL 3.7884 mL
    20 mM 0.1137 mL 0.5683 mL 1.1365 mL 2.8413 mL
    25 mM 0.0909 mL 0.4546 mL 0.9092 mL 2.2730 mL
    30 mM 0.0758 mL 0.3788 mL 0.7577 mL 1.8942 mL
    40 mM 0.0568 mL 0.2841 mL 0.5683 mL 1.4206 mL
    50 mM 0.0455 mL 0.2273 mL 0.4546 mL 1.1365 mL
    60 mM 0.0379 mL 0.1894 mL 0.3788 mL 0.9471 mL
    80 mM 0.0284 mL 0.1421 mL 0.2841 mL 0.7103 mL
    100 mM 0.0227 mL 0.1137 mL 0.2273 mL 0.5683 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    PF-06424439 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:

    PF-064244391469284-78-3PF06424439PF 06424439AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    PF-06424439
    Cat. No.:
    HY-108341
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.