| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Clorindione targets vitamin K-dependent clotting factors by acting as a vitamin K antagonist. It inhibits the synthesis of vitamin K-dependent clotting factors in the liver, thereby lowering prothrombin levels and preventing blood clot formation. The compound also shows activity against arachidonate 5-lipoxygenase with an IC50 of 5.30 (‑log[M]). By interfering with the vitamin K epoxide reductase cycle, Clorindione depletes the reduced form of vitamin K required for the γ-carboxylation of glutamic acid residues on clotting factors II, VII, IX, and X.
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| ln Vitro |
In vitro, Clorindione acts as a potent anticoagulant by inhibiting the synthesis of vitamin K-dependent clotting factors. Its activity can be assessed by measuring the prolongation of clotting time in plasma samples. The compound's inhibitory effect on arachidonate 5-lipoxygenase has also been characterized with an IC50 value of 5.30 (‑log[M]), suggesting additional anti-inflammatory properties beyond its primary anticoagulant effect.
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| ln Vivo |
In vivo, Clorindione effectively reduces blood coagulation and prolongs clotting time by lowering prothrombin levels in the bloodstream. It was previously used clinically for the prevention and treatment of thromboembolic disorders. The compound's anticoagulant effect is dose-dependent and requires monitoring of prothrombin time to maintain therapeutic efficacy while avoiding bleeding complications.
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| Enzyme Assay |
In cell-free enzymatic assays, Clorindione's activity can be evaluated by measuring its inhibition of vitamin K epoxide reductase or arachidonate 5-lipoxygenase. For the lipoxygenase assay, the enzyme is incubated with arachidonic acid substrate in the presence of varying concentrations of Clorindione, and the production of 5-HETE is quantified by HPLC. The IC50 is calculated from the concentration-response curve.
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| Cell Assay |
In vitro cell-based experiments with Clorindione typically involve culturing hepatocytes or plasma samples to assess its effect on clotting factor synthesis. Cells are treated with various concentrations of the compound, and the levels of vitamin K-dependent clotting factors (II, VII, IX, X) are measured by ELISA or functional coagulation assays. The prolongation of prothrombin time is used as a readout of anticoagulant activity.
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| Animal Protocol |
In vivo animal experiments with Clorindione have been conducted in rodent models to evaluate its anticoagulant efficacy. Animals are administered the compound orally or intravenously at various doses, and blood samples are collected at multiple time points. Prothrombin time and activated partial thromboplastin time are measured to assess the extent of anticoagulation. The compound's effects on thrombus formation can be evaluated in models of venous or arterial thrombosis.
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| ADME/Pharmacokinetics |
Clorindione is an orally active anticoagulant. Its pharmacokinetic properties include absorption from the gastrointestinal tract and distribution to the liver, where it exerts its pharmacological effect. The compound is metabolized in the liver and excreted primarily via the kidneys. Its half-life and bioavailability are characteristic of indandione-class anticoagulants, though specific parameters are not well documented in the available literature.
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| Toxicity/Toxicokinetics |
In preclinical toxicity studies, Clorindione's primary adverse effect is bleeding due to its anticoagulant mechanism, similar to other vitamin K antagonists. Overdose can lead to hemorrhage, which may be reversed by vitamin K administration. No specific organ toxicity has been reported at therapeutic doses. The compound is for research use only and is not intended for human therapeutic use.
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| Additional Infomation |
Clarindione is a cyclic ketone belonging to the indanone class of compounds. It is a vitamin K antagonist and may help lower prothrombin levels in the body.
Clorindione has a molecular formula of C15H9ClO2 and a molecular weight of 256.68. Its IUPAC name is 2-(4-chlorophenyl)indene-1,3-dione. It is also known as Chlorindione and Chlophenadione. The compound was previously marketed in Europe for thromboembolic disorders but has been largely replaced by warfarin derivatives due to better safety and predictability. It is now available only for research purposes. |
| Molecular Formula |
C15H9CLO2
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|---|---|
| Molecular Weight |
256.68
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| Exact Mass |
256.029
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| CAS # |
1146-99-2
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| PubChem CID |
70846
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| Appearance |
White to off-white solid powder
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| Density |
1.367g/cm3
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| Boiling Point |
434.7ºC at 760mmHg
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| Melting Point |
142-144ºC
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| Flash Point |
183.4ºC
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| Vapour Pressure |
2.32E-08mmHg at 25°C
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| Index of Refraction |
1.706
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| LogP |
3.502
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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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| SMILES |
O=C1C(C2=CC=C(Cl)C=C2)C(C3=C1C=CC=C3)=O
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| InChi Key |
NJDUWAXIURWWLN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H9ClO2/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-chlorophenyl)indene-1,3-dione
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| Synonyms |
Chlorindionum; Chlor-athrombon; Clorindione
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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 : ~100 mg/mL (~389.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8959 mL | 19.4795 mL | 38.9590 mL | |
| 5 mM | 0.7792 mL | 3.8959 mL | 7.7918 mL | |
| 10 mM | 0.3896 mL | 1.9480 mL | 3.8959 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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