| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular target of warfarin potassium is vitamin K epoxide reductase (VKOR), specifically the VKORC1 subunit. By inhibiting VKOR, warfarin prevents the recycling of vitamin K epoxide back to its reduced form, leading to decreased γ-carboxylation and reduced activity of clotting factors II, VII, IX, and X.
|
|---|---|
| ln Vitro |
Warfarin inhibits VKORC1 with an IC50 of 24.7 nM in cell-based assays using HEK293T cells co-expressing human Factor IX and wild-type VKORC1. In vitro assays with microsomal VKORC1 yield IC50 values of 52 nM (GSH as reductant) and 2.4 μM (DTT as reductant).
|
| ln Vivo |
Warfarin potassium is an orally active anticoagulant that effectively prevents thrombus formation in vivo. In animal models, warfarin administration leads to prolonged prothrombin time and activated partial thromboplastin time. It is used clinically for the prevention and treatment of thromboembolic disorders.
|
| Enzyme Assay |
The VKORC1 activity assay for warfarin uses recombinant VKORC1 or microsomal preparations. The assay measures the reduction of vitamin K epoxide to vitamin K in the presence of DTT or GSH as a reducing agent. Vitamin K production is quantified by HPLC or fluorescence. Warfarin is pre-incubated with the enzyme before initiating the reaction.
|
| Cell Assay |
Cell-based assays for warfarin use HEK293T cells co-expressing human Factor IX and wild-type VKORC1. Cells are treated with warfarin for 24-48 hours, and the γ-carboxylation status of Factor IX in the culture medium is assessed by ELISA using a conformation-specific antibody.
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| Animal Protocol |
In vivo anticoagulation studies with warfarin use rats or rabbits. Warfarin is administered orally or intraperitoneally at doses ranging from 0.1-2 mg/kg/day. Prothrombin time and activated partial thromboplastin time are measured at regular intervals using a coagulation analyzer. The international normalized ratio is calculated to monitor anticoagulant effect.
|
| Additional Infomation |
Warfarin is an anticoagulant that works by inhibiting the synthesis of vitamin K-dependent clotting factors. It is indicated for the prevention and/or treatment of venous thrombosis and its spread, pulmonary embolism, and atrial fibrillation with embolism. Warfarin may also be used as adjunctive therapy for the prevention of systemic embolism after myocardial infarction. Additionally, warfarin is used as a rodenticide.
See also: Warfarin (containing active ingredient). |
| Molecular Formula |
C19H15O4-.K+
|
|---|---|
| Molecular Weight |
346.4183
|
| Exact Mass |
308.105
|
| CAS # |
2610-86-8
|
| Related CAS # |
129-06-6 (sodium);81-81-2 (free acid);2610-86-8 (potassium);
|
| PubChem CID |
23706212
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.307g/cm3
|
| Boiling Point |
515.2ºC at 760mmHg
|
| Flash Point |
188.8ºC
|
| LogP |
3.609
|
| tPSA |
67.51
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
24
|
| Complexity |
508
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[K+].CC(CC(C1C(=O)OC2=CC=CC=C2C=1[O-])C1C=CC=CC=1)=O
|
| InChi Key |
WSHYKIAQCMIPTB-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C19H16O4.K/c1-12(20)11-15(13-7-3-2-4-8-13)17-18(21)14-9-5-6-10-16(14)23-19(17)22;/h2-10,15,21H,11H2,1H3;/q;+1/p-1
|
| Chemical Name |
potassium;2-oxo-3-(3-oxo-1-phenylbutyl)chromen-4-olate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8867 mL | 14.4333 mL | 28.8667 mL | |
| 5 mM | 0.5773 mL | 2.8867 mL | 5.7733 mL | |
| 10 mM | 0.2887 mL | 1.4433 mL | 2.8867 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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