PF-06424439
Based on 27 publication(s) in Google Scholar
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.
- Purity: 99.98%
- CAS No.: 1469284-78-3
- Formula: C22H26ClN7O
- Molecular Weight:439.94
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) PF-06424439
More- Cancer Cell. 2026 Feb 9;44(2):383-404.e18. [Abstract]
- Nat Neurosci. 2026 Jun 26. [Abstract]
- Nat Commun. 2024 Sep 27;15(1):8273. [Abstract]
- Adv Sci (Weinh). 2025 May 14:e2406150. [Abstract]
- Theranostics. 2024 Jun 1;14(9):3470-3485. [Abstract]
- Protein Cell. 2025 Nov 19:pwaf101. [Abstract]
- Cell Death Dis. 2025 Oct 7;16(1):715. [Abstract]
- Int J Biol Macromol. 2024 Dec;282(Pt 5):137235. [Abstract]
- Anal Chem. 2025 Jul 22;97(28):15393-15401. [Abstract]
- Mol Metab. 2024 Jun:84:101953. [Abstract]
- mBio. 2026 Apr 8;17(4):e0336825. [Abstract]
- Int Immunopharmacol. 2024 Jun 24:138:112518. [Abstract]
- J Dairy Sci. 2024 Jun 6:S0022-0302(24)00897-X. [Abstract]
- J Dairy Sci. 2022 Apr;105(4):3588-3600. [Abstract]
- FASEB J. 2025 Nov 30;39(22):e71249. [Abstract]
- J Biol Chem. 2024 Apr;300(4):107168. [Abstract]
- J Virol. 2022 Jan 26;96(2):e0147321. [Abstract]
- Cell Signal. 2026 Jun:142:112454. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2025 Aug 22;1870(8):159683. [Abstract]
- Dev Comp Immunol. 2021 Nov:124:104197. [Abstract]
- bioRxiv. 2026 Jun 11:2026.06.10.731372. [Abstract]
- bioRxiv. 2026 Mar 13.
- bioRxiv. 2026 Mar 17.
- bioRxiv. 2025 Jul 21.
- bioRxiv. 2025 Mar 11:2025.02.18.638929. [Abstract]
- Research Square Preprint. 2024 Feb 12.
- bioRxiv. 2023 Jul 3.
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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IF
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Cell Imaging/Staining
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WB
Biological Activity
IC50: 14 nM (DGAT2)[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.
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Animal Model:Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)[1]
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Dosage:60 mg/kg
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Administration:P.o.; daily; for 3 days
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Result:Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids.
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Animal Model:Male Wistar-Han rats[1]
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Dosage:1 mg/kg
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Administration:I.v.
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Result:Showed moderate clearance and a short half-life with t1/2=1.39 h.
Chemical Information
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CAS No. 1469284-78-3
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Appearance Solid
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Molecular Weight 439.94
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Formula C22H26ClN7O
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Color White to off-white
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SMILES
O=C([C@H]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (27)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Multiomic integration reveals tumoral heterogeneity of lipid dependence within lethal group 3 medulloblastoma. [Abstract]2026 Feb 9;44(2):383-404.e18. PMID: 41544627
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.
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Nat Neurosci
The mitochondrial unfolded protein response in human microglia disrupts neuronal-glial communication and promotes senescence. [Abstract]2026 Jun 26. PMID: 42362883 -
Nat Commun
Lipid droplets sequester palmitic acid to disrupt endothelial ciliation and exacerbate atherosclerosis in male mice. [Abstract]2024 Sep 27;15(1):8273. PMID: 39333556
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.
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Adv Sci (Weinh)
Lipid Droplet-Derived Biomimetic Nanocarriers for the Enhancement of Porcine Intermuscular Fat Content. [Abstract]2025 May 14:e2406150. PMID: 40365640 -
Theranostics
GPAT3 is a potential therapeutic target to overcome sorafenib resistance in hepatocellular carcinoma. [Abstract]2024 Jun 1;14(9):3470-3485. PMID: 38948063 -
Protein Cell
Tumor cell-specific loss of GPX4 reprograms triacylglycerol metabolism to escape ferroptosis and impair antitumor immunity in NSCLC. [Abstract]2025 Nov 19:pwaf101. PMID: 41259048 -
Cell Death Dis
Fatty acid synthase-mediated lipid droplet formation enhances macrophage killing of Staphylococcus aureus. [Abstract]2025 Oct 7;16(1):715. PMID: 41057302 -
Int J Biol Macromol
Transcription factor ETV4 plays a critical role in the development of non-alcoholic fatty liver disease. [Abstract]2024 Dec;282(Pt 5):137235. PMID: 39500423 -
Anal Chem
2025 Jul 22;97(28):15393-15401. PMID: 40557718 -
Mol Metab
Long-chain acyl-CoA synthetase-4 regulates endometrial decidualization through a fatty acid β-oxidation pathway rather than lipid droplet accumulation. [Abstract]2024 Jun:84:101953. PMID: 38710444
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.
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mBio
African swine fever virus hijacks lipolysis induced by chaperone-mediated autophagy to upregulate fatty acid β-oxidation and promote viral replication. [Abstract]2026 Apr 8;17(4):e0336825. PMID: 41801037 -
Int Immunopharmacol
Targeting lipid peroxidation-associated ferroptosis suppresses lung carcinoma progression by regulating cell cycle arrest. [Abstract]2024 Jun 24:138:112518. PMID: 38917528 -
J Dairy Sci
Diacylglycerol O-acyltransferase (DGAT) isoforms play a role in peridroplet mitochondrial fatty acid metabolism in bovine liver. [Abstract]2024 Jun 6:S0022-0302(24)00897-X. PMID: 38851581 -
J Dairy Sci
Role of diacylglycerol O-acyltransferase (DGAT) isoforms in bovine hepatic fatty acid metabolism. [Abstract]2022 Apr;105(4):3588-3600. PMID: 35181144
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).
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FASEB J
FOXA1 Upregulates HILPDA to Enhance Lipid Droplet Accumulation and Anoikis Resistance in Lung Adenocarcinoma. [Abstract]2025 Nov 30;39(22):e71249. PMID: 41246996
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).
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J Biol Chem
Neuroinvasive virus facilitates viral replication by employing lipid droplets to reduce arachidonic acid-induced ferroptosis. [Abstract]2024 Apr;300(4):107168. PMID: 38490434 -
J Virol
Lipid Droplets Are Beneficial for Rabies Virus Replication by Facilitating Viral Budding. [Abstract]2022 Jan 26;96(2):e0147321. PMID: 34757839
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).
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Cell Signal
2026 Jun:142:112454. PMID: 41765311 -
Biochim Biophys Acta Mol Cell Biol Lipids
Modulation of lipid droplet biogenesis by p38 MAPK and caspase-1 in docosahexaenoic acid-induced EA.hy926 endothelial cell apoptosis. [Abstract]2025 Aug 22;1870(8):159683. PMID: 40850528 -
Dev Comp Immunol
ATF6-DGAT pathway is involved in TLR7-induced innate immune response in Ctenopharyngodon idellus kidney cells. [Abstract]2021 Nov:124:104197. PMID: 34228994
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.
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bioRxiv
2026 Jun 11:2026.06.10.731372. PMID: 42327215 -
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bioRxiv
Regulation of lipid dysmetabolism and neuroinflammation progression linked with Alzheimer's disease through modulation of Dgat2. [Abstract]2025 Mar 11:2025.02.18.638929. PMID: 40027815 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (251 KB)
- 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. [Content Brief]
[2]. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010. [Content Brief]
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 |