| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Bromindione targets vitamin K epoxide reductase (VKOR), the enzyme responsible for regenerating reduced vitamin K, which is essential for the post-translational carboxylation of vitamin K-dependent clotting factors (factors II, VII, IX, and X). By inhibiting VKOR, bromindione prevents the hepatic synthesis of functional clotting factors, leading to reduced blood coagulation and prolonged prothrombin time.
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|---|---|
| ln Vitro |
In vitro, bromindione acts as a vitamin K antagonist by inhibiting vitamin K epoxide reductase activity in liver microsomal preparations. The compound shows potent anticoagulant activity in plasma-based coagulation assays, including prothrombin time (PT) and international normalized ratio (INR) measurements. It demonstrates concentration-dependent prolongation of clotting times. The compound's indandione structure distinguishes it from coumarin-based anticoagulants.
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| ln Vivo |
In vivo, bromindione is a potent and long-acting oral anticoagulant. Following oral administration, it inhibits hepatic synthesis of vitamin K-dependent clotting factors, resulting in prolonged prothrombin time and reduced blood coagulation. Its long-acting nature makes it effective as a rodenticide. The compound has been used in both human medicine as an anticoagulant and in pest control applications.
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| Enzyme Assay |
For non-cell enzyme/receptor binding assays, bromindione activity is assessed using liver microsome preparations containing vitamin K epoxide reductase. The compound is incubated with microsomes, vitamin K epoxide, and NADPH. Enzyme activity is measured by monitoring the conversion of vitamin K epoxide to vitamin K quinone using HPLC or radiometric methods. Inhibition curves are generated to determine IC₅₀ values for VKOR inhibition.
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| Cell Assay |
For in vitro cell-based assays, bromindione activity can be assessed in cultured hepatocytes or liver cell lines. Cells are treated with various concentrations of the compound, and the production of vitamin K-dependent clotting factors is measured by ELISA or functional coagulation assays. The effect on cellular VKOR activity can also be assessed by measuring the carboxylation status of vitamin K-dependent proteins. Coagulation factor levels are determined from cell culture supernatants.
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| Animal Protocol |
For in vivo animal experiments, bromindione is typically administered orally to rodents or other test animals. Prothrombin time is measured at various time points following administration to assess anticoagulant efficacy. Dose-response studies are conducted to determine the minimum effective dose and duration of action. The compound's long-acting nature is evaluated by monitoring coagulation parameters over extended periods post-administration.
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| ADME/Pharmacokinetics |
Bromindione has a molecular weight of 301.14 g/mol and molecular formula C₁₅H₉BrO₂. It is a synthetic indandione derivative. The compound is administered orally and has a long duration of action due to its mechanism of inhibiting vitamin K regeneration. Its pharmacokinetic profile is characterized by good oral bioavailability and extensive plasma protein binding. The compound is metabolized in the liver and excreted in urine.
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| Toxicity/Toxicokinetics |
Bromindione toxicity is associated with its anticoagulant effect, and overdose can lead to severe bleeding complications. As a vitamin K antagonist, it can cause hemorrhage, bruising, and prolonged bleeding time. The compound is used as a rodenticide due to its ability to cause fatal hemorrhage in rodents. In humans, it should be used with careful monitoring of coagulation parameters. Vitamin K is the antidote for bromindione poisoning.
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| Additional Infomation |
Bromindione belongs to the indanone class of compounds and is a cyclic ketone.
Bromindione was introduced as an oral anticoagulant in the 1960s under the INN name bromindione (p-INNList-12, 1962; r-INNList-5, 1965). It belongs to the indandione class of anticoagulants and is structurally related to phenindione. The compound has been used both therapeutically as an anticoagulant and as a rodenticide. Its use in human medicine has largely been superseded by newer anticoagulants, but it remains a compound of interest in research. |
| Molecular Formula |
C15H9O2BR
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|---|---|
| Molecular Weight |
301.13476
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| Exact Mass |
299.979
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| CAS # |
1146-98-1
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| PubChem CID |
14369
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| Appearance |
Light brown to brown solid powder
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| Density |
1.569g/cm3
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| Boiling Point |
450.1ºC at 760 mmHg
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| Flash Point |
151.2ºC
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| Vapour Pressure |
2.72E-08mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
3.611
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
334
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NPUZIGSOEWMFKK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H9BrO2/c16-10-7-5-9(6-8-10)13-14(17)11-3-1-2-4-12(11)15(13)18/h1-8,13H
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| Chemical Name |
2-(4-bromophenyl)indene-1,3-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~830.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (20.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3208 mL | 16.6041 mL | 33.2082 mL | |
| 5 mM | 0.6642 mL | 3.3208 mL | 6.6416 mL | |
| 10 mM | 0.3321 mL | 1.6604 mL | 3.3208 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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