Perfluoro(2-methyl-3-oxahexanoic) acid
Based on 1 publication(s) in Google Scholar
Perfluoro (2-methyl-3-oxahexanoic) acid (HFPO-DA) is an orally active PPARα agonist with an EC50 of 2.1 μM for human PPARα. Perfluoro (2-methyl-3-oxahexanoic) acid induces peroxisome proliferation and increases the levels of proinflammatory mediators. It impairs intestinal barrier function and disrupts cecal flora balance. Perfluoro (2-methyl-3-oxahexanoic) acid is applicable to research related to developmental toxicity, hepatotoxicity and intestinal toxicity.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 13252-13-6
- Formula: C6HF11O3
- Molecular Weight:330.05
-
Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Perfluoro(2-methyl-3-oxahexanoic) acid
More
Biological Activity
|
PPARα 2.1 μM (EC50) |
Perfluoro(2-methyl-3-oxahexanoic) acid (HFPO-DA) activates mouse PPARα in a transactivation reporter gene assay with an EC50 of 40 μM[1].
Perfluoro(2-methyl-3-oxahexanoic) acid activates rat PPARα in transactivation reporter gene assays with an EC50 of 114 μM and an EC20 of 83.18 μM, and is more potent than endogenous fatty acids and clofibric acid[1].
Perfluoro(2-methyl-3-oxahexanoic) acid fully activates human PPARα in a transactivation reporter gene assay with an EC50 of 2.1 μM and 134% efficacy relative to positive control[1].
Perfluoro(2-methyl-3-oxahexanoic) acid induces hepatic lipid metabolism-related gene expression in HepG2 human hepatoma cells[1].
Perfluoro(2-methyl-3-oxahexanoic) acid (1 mM) weakly activates mouse PPARγ in a transactivation reporter gene assay, with minimal binding affinity to the PPARγ ligand binding domain[1].
Perfluoro(2-methyl-3-oxahexanoic) acid (300 μM) activates rat PPARγ (GAL4 fusion construct) with a lowest observed effect concentration of 300 μM, yielding a 2-fold increase over vehicle control[1].
Perfluoro(2-methyl-3-oxahexanoic) acid (Environmental levels) significantly inhibits chlorella growth and alters chlorella antioxidant responses in cell-free in vitro assays[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Perfluoro(2-methyl-3-oxahexanoic) acid (50 mg/kg male, 500 mg/kg female; p.o.; daily; chronic) induces tumors in Sprague Dawley rats in a pattern consistent with the PPARα activator tumor triad, with liver tumors in females at 500 mg/kg-day and pancreatic/Leydig cell tumors in males at 50 mg/kg-day[1].
Perfluoro(2-methyl-3-oxahexanoic) acid (5-500 μg/L; aqueous exposure; continuous; 120 hours) induces significant developmental toxicity in Danio rerio embryos, including increased heart rate, inhibited locomotor activity, altered antioxidant and neurotoxicity-related enzyme activities, disrupted HPT axis function, modified apoptosis-related gene expression, and impaired lipid metabolism gene regulation[2].
Perfluoro(2-methyl-3-oxahexanoic) acid (2-200 μg/L; p.o.; daily; 6 weeks) induces dose-dependent intestinal inflammation, colonic barrier dysfunction, and gut microbiota disruption in male C57BL/6J mice, with the 200 μg/L dose producing the most robust and broad toxic effects[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:male, female, pregnant dams[1]
-
Dosage:0.1 mg/kg (28/90 days); 0.5 mg/kg (90 days); 1 mg/kg (28 days); 2 mg/kg (gestation days 1.5-17.5); 3 mg/kg (28 days); 5 mg/kg (90 days/gestation days 1.5-17.5); 10 mg/kg (gestation days 1.5-17.5); 30 mg/kg (28 days)
-
Administration:p.o.; daily; 28 days, 90 days, or gestation days 1.5-17.5
-
Result:Increased PPARα signaling and peroxisomal lipid metabolism signaling, and caused hepatocellular hypertrophy and hepatomegaly at 0.5 mg/kg after 90 days.
Increased PPARα signaling, and caused hepatocellular hypertrophy and hepatomegaly at 1 mg/kg after 28 days.
Caused large, statistically significant increase in peroxisomal β-oxidation activity, hepatocellular hypertrophy, single cell necrosis/apoptosis, and increased mitotic cell cycle signaling at 3 mg/kg after 28 days.
Caused increased mitotic figures in liver tissue at 2 and 10 mg/kg in pregnant dams after gestation days 1.5-17.5.
Increased peroxisomal β-oxidation activity, and caused hepatocellular hypertrophy, mitotic figures, single cell necrosis/apoptosis at 30 mg/kg after 28 days.
-
Animal Model:Sprague Dawley (male, female)[1]
-
Dosage:50 mg/kg (male rats); 500 mg/kg (female rats)
-
Administration:p.o.; daily; chronic
-
Result:Induced liver tumors in female rats at 500 mg/kg-day.
Caused a small but statistically significant increase in pancreatic acinar cell adenomas/carcinomas and a slight elevation in Leydig cell tumors, and showed liver effects consistent with PPARα activation in male rats at 50 mg/kg-day.
-
Animal Model:C57BL/6J (6-week-old male)[3]
-
Dosage:2 μg/L (average 0.3 μg/kg/day); 20 μg/L (average 3 μg/kg/day); 200 μg/L (average 30 μg/kg/day)
-
Administration:p.o.; daily; 6 weeks
-
Result:Increased serum TNF-α levels, increased ileal TNF-α mRNA levels, decreased colon Mep1A mRNA levels and colon Mep1B mRNA levels, decreased ileal MUC2 mRNA levels, and decreased fecal Firmicutes relative abundance at 2 μg/L dose.
Increased ileal TNF-α mRNA levels and ileal IL-1β mRNA levels, decreased colon Mep1B mRNA levels, increased colon Occludin mRNA levels, increased ileal KLF4 mRNA levels and ileal FABP2 mRNA levels, increased colon TLR4 protein levels, and decreased fecal Firmicutes relative abundance at 20 μg/L dose.
Chemical Information
-
CAS No. 13252-13-6
-
Appearance Liquid (Density: 1.69 g/cm3)
-
Molecular Weight 330.05
-
Formula C6HF11O3
-
Color Colorless to light yellow
-
SMILES
O=C(O)C(OC(F)(F)C(F)(F)C(F)(F)F)(F)C(F)(F)F
-
Synonyms
HFPO-DA
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Toxicology
ALDH1A3-dependent ferroptosis mediates hexafluoropropylene oxide dimer acid-induced trophoblast dysfunction. [Abstract]2026 Sep:525:154505. PMID: 42176843
Solvent & Solubility
DMSO : 100 mg/mL (302.98 mM; Need ultrasonic; 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 (7.57 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 (7.57 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Data Sheet (281 KB)
-
SDS (477 KB)
- English - EN (477 KB)
- Français - FR (477 KB)
- Deutsch - DE (477 KB)
- Norwegian - NO (477 KB)
- Español - ES (477 KB)
- Swedish - SV (477 KB)
- Italian - IT (477 KB)
- Korean - KR (477 KB)
- Portuguese - PT (477 KB)
-
Handling Instructions (2659 KB)
References
[1]. Heintz MM, et al. Assessment of the mode of action underlying development of liver lesions in mice following oral exposure to HFPO-DA and relevance to humans. Toxicol Sci. 2023;192(1):15-29. [Content Brief]
[2]. Wang Y, et al. Comparison of developmental toxicity induced by PFOA, HFPO-DA, and HFPO-TA in zebrafish embryos. Chemosphere. 2023;311(Pt 1):136999. [Content Brief]
[3]. Xie X, et al. Exposure to hexafluoropropylene oxide dimer acid (HFPO-DA) disturbs the gut barrier function and gut microbiota in mice. Environ Pollut. 2021;290:117934. [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 | 3.0298 mL | 15.1492 mL | 30.2984 mL | 75.7461 mL |
| 5 mM | 0.6060 mL | 3.0298 mL | 6.0597 mL | 15.1492 mL | |
| 10 mM | 0.3030 mL | 1.5149 mL | 3.0298 mL | 7.5746 mL | |
| 15 mM | 0.2020 mL | 1.0099 mL | 2.0199 mL | 5.0497 mL | |
| 20 mM | 0.1515 mL | 0.7575 mL | 1.5149 mL | 3.7873 mL | |
| 25 mM | 0.1212 mL | 0.6060 mL | 1.2119 mL | 3.0298 mL | |
| 30 mM | 0.1010 mL | 0.5050 mL | 1.0099 mL | 2.5249 mL | |
| 40 mM | 0.0757 mL | 0.3787 mL | 0.7575 mL | 1.8937 mL | |
| 50 mM | 0.0606 mL | 0.3030 mL | 0.6060 mL | 1.5149 mL | |
| 60 mM | 0.0505 mL | 0.2525 mL | 0.5050 mL | 1.2624 mL | |
| 80 mM | 0.0379 mL | 0.1894 mL | 0.3787 mL | 0.9468 mL | |
| 100 mM | 0.0303 mL | 0.1515 mL | 0.3030 mL | 0.7575 mL |