Product Introduction
Dicoumarol is a naturally occurring coumarin derivative originally isolated from spoiled sweet clover and identified as the causative agent of hemorrhagic sweet clover disease in cattle. It functions as a potent competitive inhibitor of vitamin K epoxide reductase (VKOR), thereby blocking the regeneration of reduced vitamin K and inhibiting the synthesis of functional vitamin K-dependent coagulation factors. Beyond its well-established anticoagulant activity, dicoumarol has been identified as an inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1), an enzyme overexpressed in many solid tumors that plays a role in maintaining cellular redox homeostasis and mediating chemoresistance. Through NQO1 inhibition, dicoumarol sensitizes cancer cells to chemotherapeutic agents and induces oxidative stress. Additionally, dicoumarol has been shown to modulate the activity of the aryl hydrocarbon receptor and exhibits antibacterial and antiviral properties, making it a valuable tool in cancer biology, redox biochemistry, and pharmacological research.
Product Features
1. Potent NQO1 Inhibitor: Competitive inhibitor of NAD(P)H:quinone oxidoreductase 1, widely used to study NQO1 function in cancer redox biology and chemoresistance.
2. Dual Pharmacological Activity: Inhibits both VKOR (anticoagulant effect) and NQO1, providing a tool for investigating vitamin K-dependent processes and cellular quinone metabolism.
3. Natural Coumarin Compound: Naturally occurring anticoagulant with well-characterized mechanism of action and extensive historical and contemporary research literature.
4. Chemosensitizing Agent: Enhances the cytotoxicity of quinone-based chemotherapeutics and oxidative stress-inducing agents in NQO1-overexpressing cancer cells.
5. High Purity: Supplied at high purity suitable for reproducible in vitro and in vivo research applications.
Specifications
Size: Available in 500 mg and 1 g
CAS Number: 66-76-2
Molecular Weight: 336.30
Molecular Formula: C19H12O6
Purity: ¡Ý98%
Solubility: DMSO: ¡Ý10 mg/mL; aqueous buffers: limited solubility; soluble in alkaline solutions
Storage and Stability
Storage Conditions: Store at room temperature (15-25¡ãC) in a tightly sealed container, protected from light and moisture.
Shelf Life: The product is stable for 36 months from the date of manufacture when stored as directed.
Protocol (For Reference Only)
Important: Dicoumarol is light-sensitive. Prepare stock solutions freshly and protect from light during handling and storage.
1. Stock Solution Preparation: Dissolve dicoumarol in DMSO to prepare a concentrated stock solution (e.g., 10-100 mM). For aqueous applications, dissolve in alkaline buffer (pH 8.0-9.0) with gentle warming. Aliquot stock solutions and store at -20¡ãC protected from light.
2. In Vitro Working Solution Preparation: Dilute DMSO stock solution into culture medium or assay buffer to achieve working concentrations typically ranging from 10-200 µM depending on cell type and experimental endpoint.
3. NQO1 Inhibition in Cell Culture: For NQO1 inhibition studies, pretreat cells with dicoumarol at 50-200 µM for 1-4 hours before addition of NQO1 substrates or chemotherapeutic agents. Assess NQO1 activity by measuring the reduction of menadione or other NQO1 substrates.
4. Chemosensitization Assays: Combine dicoumarol (50-200 µM) with quinone-based chemotherapeutics such as ¦Â-lapachone or mitomycin C to evaluate synergistic cytotoxic effects in NQO1-overexpressing cancer cell lines. Assess cell viability by MTT or clonogenic survival assays.
5. Redox and Oxidative Stress Assessment: Following dicoumarol treatment, evaluate intracellular reactive oxygen species levels using fluorescent probes such as DCFH-DA, and measure markers of oxidative stress and DNA damage by Western blot or immunofluorescence.
Precautions
1. Protect from light during handling and storage; dicoumarol is photodegradable and exposure to light reduces potency.
2. Dicoumarol has limited solubility in neutral aqueous solutions; prepare stock solutions in DMSO or alkaline buffer for best results.
3. Use appropriate vehicle controls in all experiments. DMSO concentration in cell culture medium should not exceed 0.1-0.2% to avoid solvent-related cytotoxicity.
4. Dicoumarol is a known anticoagulant and exhibits toxicity at elevated concentrations; handle with appropriate safety precautions and consult the Safety Data Sheet before use.
5. For research use only. Not for use in diagnostic or therapeutic procedures.
FAQ (Simplified)
Q1: What is the recommended starting concentration for NQO1 inhibition in vitro?
A1: Dicoumarol at 50-200 µM effectively inhibits NQO1 in most cell types. For complete inhibition, 200 µM is commonly used. Perform dose-response experiments to determine optimal concentrations for specific cell lines and assays.
Q2: How should I dissolve dicoumarol for aqueous assays?
A2: For aqueous applications, dissolve dicoumarol in alkaline solution (pH 8.0-9.0) or prepare concentrated stock in DMSO followed by dilution into assay buffer. Limit final DMSO concentration to ¡Ü0.1% in cell culture.
Q3: Does dicoumarol affect pathways other than NQO1?
A3: Yes. Dicoumarol also inhibits VKOR (anticoagulant effect) and may modulate aryl hydrocarbon receptor signaling. Consider these pleiotropic effects when designing experiments and interpreting results.
Q4: Can dicoumarol be used in vivo?
A4: Dicoumarol has been used in rodent models at doses ranging from 10-30 mg/kg via intraperitoneal or oral administration. Due to its anticoagulant activity, careful dose optimization and monitoring of coagulation parameters are recommended. Consult literature for established protocols specific to your experimental model.
Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions using a small-scale pilot experiment is strongly recommended before processing valuable samples.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages, including loss of samples or data.
4. Wear appropriate protective clothing and gloves when handling this product. Dicoumarol is a biologically active anticoagulant; review the Safety Data Sheet before handling.
Ordering Information
Catalog Number: IC-02105532
Product Name: Dicoumarol
Size: 500 mg / 1 g
Price: 
500 mg: CNY ¥800.00 / USD $80.00 / EUR €96.00 / JPY ¥14400.00
1 g: CNY ¥1250.00 / USD $125.00 / EUR €150.00 / JPY ¥22500.00
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