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Esculetin Lipoxygenase inhibitor

Name: Esculetin
SKU: S4711
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4711

Esculetin (Cichorigenin, Aesculetin) is a coumarin derivative found in various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs).

Chemical Structure

Molecular Weight: 178.14

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

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Chemical Information, Storage & Stability

Molecular Weight	178.14	Formula	C₉H₆O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	305-01-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Cichorigenin, Aesculetin			Smiles	C1=CC(=O)OC2=CC(=C(C=C21)O)O

Solubility

In vitro
Batch:

DMSO : 35 mg/mL (196.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10mg/ml (56.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	lipoxygenase ^[2]
In vitro	Esculetin decreases cell proliferation by inducing G1 phase cell cycle arrest, which is associated with the down-regulation of cyclin D1/CDK4 and cyclin E/CDK2 complexes by the activation of p27KIP^[2]. This compound significantly inhibits proliferation of HCC cells in a concentration- and time-dependent manner and with an IC50 value of 2.24 mM. It blocks the cell cycle at S phase and induces apoptosis in SMMC-7721 cells with significant elevation of caspase-3 and caspase-9 activity, but does not affect caspase-8 activity. This chemical treatment results in the collapse of mitochondrial membrane potential in vitro and in vivo accompanied by increased Bax expression and decreased Bcl-2 expression at both transcriptional and translational levels. It exerts in vitro and in vivo antiproliferative activity in hepatocellular carcinoma, and its mechanisms involved initiation of a mitochondrial-mediated, caspase-dependent apoptosis pathway^[3].
In vivo	Esculetin significantly decreases tumor growth in mice bearing Hepa1-6 cells. Tumor weight is decreased by 20.33, 40.37, and 55.42% with increasing doses of this compound. Of note, it has no obvious toxicity in this animal study^[3]. In a rat experimental model of inflammatory bowel disease induced by trinitrobenzenesulfonic acid, this compound at the dose of 5 mg/kg displays intestinal anti-inflammatory activity^[4].
References	[1] https://pubmed.ncbi.nlm.nih.gov/17062797/ [2] https://pubmed.ncbi.nlm.nih.gov/21109980/ [3] https://pubmed.ncbi.nlm.nih.gov/25517918/ [4] http://eji.sagepub.com/content/11/2/433.short

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