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Chemical Structure| 305-01-1 Chemical Structure| 305-01-1

Structure of Esculetin
CAS No.: 305-01-1

Chemical Structure| 305-01-1

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Esculetin is a naturally occuring 5-lipoxygenase and 12-Lipoxygenase inhibitor with IC50 values of ID50 values of 4 and 2.5 µM, respectively.

Synonyms: Cichorigenin; Aesculetin; NSC 26428

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Product Details of Esculetin

CAS No. :305-01-1
Formula : C9H6O4
M.W : 178.14
SMILES Code : O=C1C=CC2=C(O1)C=C(O)C(O)=C2
Synonyms :
Cichorigenin; Aesculetin; NSC 26428
MDL No. :MFCD00006874

Safety of Esculetin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Esculetin

RTK

Isoform Comparison

Biological Activity

Target
  • lipoxygenase

In Vitro:

Cell Line
Concentration Treated Time Description References
colonic crypt epithelium 500 μM 10 minutes Completely abolished DOC-induced increases in chemiluminescence (CL) J Clin Invest. 1986 Mar;77(3):850-9
colonic mucosal scrapings 100 μM 10 minutes Suppressed basal and DOC-induced increases in chemiluminescence (CL) by 40-50%, and reduced accumulation of PGE2, LTB4, 5-HETE, 12-HETE, and 15-HETE J Clin Invest. 1986 Mar;77(3):850-9
Sorted ATMs 25 μg/mL DIL-ox-LDL 24 hours Esculetin significantly increased the percentage of CD36+ cells and CD36+ DIL-ox-LDL+ cells, indicating enhanced phagocytosis in ATMs. Theranostics. 2025 Apr 28;15(12):5910-5930
RAW 264.7 cells 25 μg/mL DIL-ox-LDL 3 to 24 hours Esculetin significantly increased the fluorescence intensity of intracellular DIL-ox-LDL, indicating enhanced phagocytosis in macrophages. Theranostics. 2025 Apr 28;15(12):5910-5930
PC12 cells 25 μM or 50 μM 24 hours Esculetin functions as an ERR agonist, enhancing glycolysis and mitochondrial respiration, leading to elevated cellular ATP levels EBioMedicine. 2017 Aug;22:225-241
Bovine chondrocytes 31 μM–500 μM 6 days Esculetin inhibited IL-1-induced cartilage degradation and significantly blocked the accumulation of ADAMTS4 and MT4-MMP proteins Osteoarthritis Cartilage. 2005 Apr;13(4):269-77
T/C28a4 chondrocytes 100–500 µM 24 hours To evaluate the inhibitory effect of Esculetin on MMP-1, MMP-3, and MMP-13 mRNA expression. Results showed that 250 µM EST reduced MMP-1, MMP-3, and MMP-13 mRNA expression to control levels, while TIMP-1 mRNA levels were unaffected. Ann Rheum Dis. 2001 Feb;60(2):158-65
Human articular cartilage cells 50–500 µM 21 days To evaluate the inhibitory effect of Esculetin on IL1 á and OSM-induced degradation in human articular cartilage. Results showed that 50 µM EST significantly inhibited proteoglycan and collagen degradation (p<0.01) and reduced MMP-1 levels (p<0.001). Ann Rheum Dis. 2001 Feb;60(2):158-65
Bovine nasal cartilage cells 10–330 µM 14 days To evaluate the inhibitory effect of Esculetin on IL1 á and OSM-induced collagen and proteoglycan degradation. Results showed that 66 µM EST significantly inhibited collagen degradation (p<0.001), and 100 µM EST significantly inhibited proteoglycan degradation (p<0.05). Ann Rheum Dis. 2001 Feb;60(2):158-65
Phytophthora sojae zoospores 100 μM 30 min To evaluate the inhibitory effect of Esculetin on the chemotaxis of Phytophthora sojae zoospores. Results showed that Esculetin competitively binds to the PsIRK1 receptor, disrupting zoospore chemotaxis toward genistein and thereby inhibiting infection. Sci Adv. 2025 Jan 10;11(2):eadt0925

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Colonic epithelial proliferation model Intracolonic instillation 50 μmol (25 mM) Single administration, observed at 4 hours (ODC activity) or 24 hours ([3H]TdR incorporation) Inhibited DOC-induced increases in ornithine decarboxylase (ODC) activity and [3H]TdR incorporation into DNA J Clin Invest. 1986 Mar;77(3):850-9
C57BL6J male mice High-fat diet-induced postprandial dyslipidemia model Oral gavage 30, 90, 180 mg/kg/d Once daily for 7 days Esculetin significantly elevated postprandial HDL cholesterol levels and increased bile acid content in bile, promoting cholesterol excretion. Theranostics. 2025 Apr 28;15(12):5910-5930
C57BL/6N Slc mice MPTP-induced Parkinson's disease model Oral 50 mg/kg/day 4 days per week for 5 months Esculetin protected dopaminergic neurons by maintaining ATP levels and reducing ER stress, mitigating Parkinson's disease symptoms EBioMedicine. 2017 Aug;22:225-241
Soybean (Glycine max) Soybean seedlings Root dipping 100 μM Single treatment, lasting 30 minutes To evaluate the preventive effect of Esculetin on Phytophthora sojae infection in soybean seedlings. Results showed that Esculetin treatment significantly increased the survival rate of soybean seedlings and reduced pathogen biomass in the roots. Sci Adv. 2025 Jan 10;11(2):eadt0925

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.61mL

1.12mL

0.56mL

28.07mL

5.61mL

2.81mL

56.14mL

11.23mL

5.61mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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