Warfarin sodium targets vitamin K epoxide reductase (VKOR) and cytochrome P450 2C9 (CYP2C9). It inhibits both vitamin K and vitamin K epoxide reductases, thereby interfering with the cyclic interconversion of vitamin K epoxide to its reduced form, vitamin KH2. The reduced form of vitamin K, vitamin KH2, is a cofactor used in the γ-carboxylation of coagulation factors II, VII, IX, and X. By inhibiting VKOR, warfarin reduces the synthesis of functional clotting factors.

In vitro, warfarin sodium inhibits vitamin K epoxide reductase (VKOR) activity. The compound's anticoagulant activity has been demonstrated in vitro using coagulation assays such as prothrombin time (PT) and international normalized ratio (INR). Warfarin sodium inhibits the γ-carboxylation of coagulation factors in cell-based assays. The compound's effects on CYP2C9 activity have been assessed using standard CYP inhibition assays.

In vivo, warfarin sodium is an effective anticoagulant agent that prevents blood clot formation. It is used to prevent and treat deep vein thrombosis, pulmonary embolism, and atrial fibrillation. Warfarin sodium decreases blood coagulation by inhibiting vitamin K epoxide reductase. The compound's anticoagulant effect is monitored by measuring prothrombin time (PT) and international normalized ratio (INR).

In vitro enzyme assays for warfarin sodium involve measuring the inhibition of vitamin K epoxide reductase (VKOR) activity. The assay typically involves incubating microsomes or purified VKOR with varying concentrations of warfarin in the presence of vitamin K epoxide. The conversion of vitamin K epoxide to vitamin K is measured using HPLC. The IC50 value is calculated. The compound's inhibition of CYP2C9 activity can be assessed using standard CYP inhibition assays with model substrates.

In vitro cell-based assays for warfarin sodium evaluate its effects on coagulation factor synthesis. Hepatocytes or other cell lines are cultured and treated with warfarin, and the production of γ-carboxylated coagulation factors is measured using ELISA or Western blot. The compound's effects on cell viability and proliferation are assessed using MTT or other assays.

In vivo, warfarin sodium is evaluated in animal models of thrombosis. Animals are treated with warfarin via oral administration, and the anticoagulant effect is assessed by measuring prothrombin time (PT) and activated partial thromboplastin time (aPTT). The compound's efficacy in preventing thrombosis is assessed in models of venous or arterial thrombosis. Pharmacokinetic studies are conducted to determine the compound's absorption, distribution, metabolism, and excretion.

Warfarin sodium is an anticoagulant agent and a vitamin K1 recycling antagonist. It has a molecular formula of C₁₉H₁₅NaO₄ and a molecular weight of 330.31 g/mol. Warfarin sodium is soluble in water and ethanol. The compound should be stored at room temperature. Warfarin sodium is a coumarin derivative that prolongs blood coagulation time.

Effects During Pregnancy and Lactation
◉ Overview of Warfarin Use During Lactation
Because the concentration of warfarin in breast milk is extremely low when the daily dose is at least 12 mg, the amount ingested by the infant is very small. Even when the mother takes 25 mg daily for 7 days during lactation, no adverse reactions have been reported in breastfed infants. It is generally believed that the risk to breastfed infants from mothers receiving warfarin treatment during lactation is minimal, and no special precautions are necessary.
The postpartum warfarin dose required by women may need to be up to twice that before pregnancy. Whether breastfeeding leads to an increased need for vitamin K is unclear.
◉ Effects on Breastfed Infants
Two infants, breastfed for 56 days and 131 days respectively, did not experience a decrease in vitamin K-dependent clotting factor levels or bleeding during their mothers' warfarin anticoagulation therapy.
In a telephone follow-up study, mothers taking warfarin reported no adverse reactions in their five breastfed infants. A mother was taking 5 mg warfarin daily for the first 7 weeks postpartum due to a pulmonary embolism. She mistakenly ingested a dose of 25 mg/day and continued this for 7 days. Upon presentation to the emergency room, her international normalized ratio (INR) was greater than 10 (the usual therapeutic upper limit is 3.5), prothrombin time was greater than 100 seconds (normal value not exceeding 11.2 seconds), and activated partial thromboplastin time (aPTT) was 62.5 seconds (normal value not exceeding 32.7 seconds). She had been exclusively breastfeeding her infant almost exclusively since birth. Her 8-week-old infant was in good health with an INR of 1.0, a prothrombin time of 10.3 seconds, and a slightly elevated aPTT of 33.8 seconds. However, 3 weeks prior, the infant's aPTT was 38.9 seconds, therefore the elevated aPTT was not determined to be caused by warfarin. ◉ Effects on breastfeeding and lactation
As of the revision date, no relevant published information was found.
The toxicity of warfarin sodium is primarily associated with its anticoagulant effect. Overdose can cause severe bleeding, including intracranial hemorrhage and gastrointestinal bleeding. The compound is teratogenic and should not be used during pregnancy. Warfarin sodium interacts with many drugs and foods, and its anticoagulant effect must be carefully monitored. The compound should be used with caution in patients with bleeding disorders or liver disease.

http://en.wikipedia.org/wiki/Warfarin

Warfarin sodium is a slightly bitter-tasting crystalline powder and an anticoagulant used as a rodenticide. (EPA, 1998)
Warfarin sodium is the sodium salt of warfarin, a coumarin compound and a vitamin K antagonist with anticoagulant activity. Warfarin sodium inhibits vitamin K and vitamin K epoxide reductase, thereby interfering with the cyclic conversion of vitamin K epoxide with its reduced form, vitamin KH2. Vitamin KH2 is a cofactor for the carboxylation of N-terminal glutamate residues in vitamin K-dependent proteins. Therefore, the maturation of vitamin K-dependent coagulation factors II, VII, IX, and X, as well as anticoagulant proteins C and S, is inhibited. The lack of these coagulation factors prevents thrombosis and clot formation.
An anticoagulant that works by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prevention and/or treatment of venous thrombosis and its spread, pulmonary embolism, and atrial fibrillation with embolism. It can also be used as an adjunct drug for the prevention of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.
See also: Warfarin (containing the active ingredient).
Warfarin sodium (Coumadin) is the sodium salt form of warfarin, a coumarin and a vitamin K antagonist with anticoagulant activity. It inhibits vitamin K epoxide reductase (VKOR) and cytochrome P450 2C9 (CYP2C9). Warfarin sodium decreases blood coagulation and prevents blood clot formation. It is used to prevent and treat blood clots in conditions such as deep vein thrombosis, pulmonary embolism, and atrial fibrillation.

C19H15NAO4

330.31477

330.086

129-06-6

129-06-6 (sodium);81-81-2 (free acid);2610-86-8 (potassium);

16204922

Solid Powder

1.307g/cm3

515.2ºC at 760mmHg

188.8ºC

4.047

0

4

4

24

508

0

CC(=O)CC(C1=CC=CC=C1)C2=C(C3=CC=CC=C3OC2=O)[O-].[Na+]

KYITYFHKDODNCQ-UHFFFAOYSA-M

InChI=1S/C19H16O4.Na/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

sodium;2-oxo-3-(3-oxo-1-phenylbutyl)chromen-4-olate

Coumadin, Aldocumar, Tedicumar, Warfant, Marevan

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)