Warfarin (WARF42; Athrombine-K; Coumadin) is an anticoagulant drug used to prevent blood clots from forming in blood vessels and spreading to other parts of the body in the event of thrombosis and thromboembolism, respectively. In addition to treating blood clots like pulmonary emboli and deep vein thrombosis, it is frequently used to treat atrial fibrillation, valvular heart disease, and artificial heart valve patients in order to prevent stroke. After orthopedic surgery and ST-segment elevation myocardial infarction, it is used less frequently. Although it is usually taken orally, injections into veins are also an option. Although more effective poisons like brodifacoum have since been developed, warfarin was first introduced in 1948 as a pesticide against rats and mice. It is still used for this purpose today. Warfarin was discovered to be a reasonably safe and effective treatment for thrombosis and thromboembolism in the early 1950s, across a wide range of disorders. Since 1954, when it was given the all-clear to be used as a medication, its popularity has not decreased. In North America, the most commonly prescribed oral anticoagulant medication is warfarin.
| Molecular Formula |
C19H16O4
|
|---|---|
| Molecular Weight |
308.33
|
| Exact Mass |
308.10
|
| Elemental Analysis |
C, 74.01; H, 5.23; O, 20.76
|
| CAS # |
81-81-2
|
| Related CAS # |
Warfarin-d5;75472-93-4
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| Appearance |
Solid powder
|
| SMILES |
CC(=O)CC(C1=CC=CC=C1)C2=C(C3=CC=CC=C3OC2=O)O
|
| InChi Key |
PJVWKTKQMONHTI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H16O4/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
|
| Chemical Name |
4-hydroxy-3-(3-oxo-1-phenylbutyl)chromen-2-one
|
| Synonyms |
WARF42; Athrombine-K; NSC 59813; NSC-59813; NSC59813; d-Con; Rat-ola; Tox-Hid; Warfarin Q
|
| HS Tariff Code |
2934.99.03.00
|
| 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) |
DMSO: ≥ 50 mg/mL (~162.2 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.11 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 (8.11 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 (8.11 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 | 3.2433 mL | 16.2164 mL | 32.4328 mL | |
| 5 mM | 0.6487 mL | 3.2433 mL | 6.4866 mL | |
| 10 mM | 0.3243 mL | 1.6216 mL | 3.2433 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03862859 | Recruiting | Drug: Warfarin | Stroke Major Bleed |
Nicholas Carlson | October 9, 2019 | Phase 4 |
| NCT03702582 | Recruiting | Drug: Warfarin Drug: Rivaroxaban |
Stroke Bleeding |
Massachusetts General Hospital | April 30, 2019 | Phase 3 |
| NCT02303171 | Recruiting | Drug: Enoxaparin Drug: Warfarin |
Recurrent Miscarriage Antiphospholipid Syndrome |
Mohamed Sayed Abdelhafez | November 2014 | Phase 4 |
| NCT05741385 | Recruiting | Drug: Caffeine Drug: Warfarin sodium |
Liver Cirrhosis | Boehringer Ingelheim | April 25, 2023 | Not Applicable |
| NCT05815680 | Active Recruiting |
Drug: warfarin Drug: IBI362 |
Overweight Subjects Obese Subjects |
Innovent Biologics (Suzhou) Co. Ltd. |
April 6, 2023 | Phase 1 |
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