(R)-(+)-Warfarin
Based on 1 Customer Validation
(R)-(+)-Warfarin is an orally active chiral 4-hydroxycoumarin compound with vitamin K epoxide reductase (VKOR) inhibitory activity and cytochrome P450 substrate activity. (R)-(+)-Warfarin undergoes stereoselective metabolism via CYP1A2 to form 6-Hydroxywarfarin and 8-Hydroxywarfarin, and is metabolized via CYP3A4 to produce 10-Hydroxywarfarin (HY-134999). (R)-(+)-Warfarin can be used for the research of thromboembolic diseases.
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- Purity: 99.55%
- CAS No.: 5543-58-8
- 화학식: C19H16O4
- 분자량:308.33
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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CYP1A2 |
CYP3A4 |
(R)-(+)-Warfarin acts as a stereoselective substrate for polymorphic recombinant human CYP450 enzymes. Wild-type CYP1A1 and its Ile462 and Val462 mutants, as well as CYP1A2, respectively catalyze the 6/8-hydroxylation of (R)-(+)-Warfarin, exhibiting differential regioselectivity and Km values. CYP2C19 mediates 8-hydroxylation but shows low expression in the liver, while CYP3A4, which has high hepatic abundance, catalyzes 10-hydroxylation and serves as the major metabolic enzyme in vivo[1].
(R)-(+)-Warfarin competitively inhibits CYP2C9-mediated metabolism of S-Warfarin in human liver microsomes, with a Ki value of 6-6.9 μM; additionally, it is stereoselectively reduced by NADPH-dependent carbonyl reductases in human liver and kidney to form R,S-warfarin alcohol, and the cytosolic enzyme fraction accounts for the majority of the reductive activity[1].
(R)-(+)-Warfarin inhibits vitamin K reductase and vitamin K1 epoxide reductase in Wistar rat liver microsomes; it is metabolized by cytochrome P-450 enzymes into multiple oxidative metabolites in human liver microsomes[2].
(R)-(+)-Warfarin binds extensively to human serum albumin, and its binding affinity is lower than that of (S)-warfarin[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(R)-(+)-Warfarin (daily; from 2 days pre-implant until study end) does not inhibit primary tumour growth or lung metastasis in mice bearing Lewis lung carcinoma, and does not produce measurable anticoagulant effects in this model[2].
(R)-(+)-Warfarin produces a longer-lasting anticoagulant response in rabbits than (S)-warfarin, even though it is less potent on a plasma concentration basis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 5543-58-8
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Appearance Solid
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분자량 308.33
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화학식 C19H16O4
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Color White to off-white
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SMILES
CC(C[C@](C1=C(O)C2=CC=CC=C2OC1=O)([H])C3=CC=CC=C3)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (162.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (4.05 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (4.05 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (788 KB)
- English - EN (788 KB)
- Français - FR (788 KB)
- Deutsch - DE (788 KB)
- Norwegian - NO (788 KB)
- Español - ES (788 KB)
- Swedish - SV (788 KB)
- Italian - IT (788 KB)
- Korean - KR (788 KB)
- Portuguese - PT (788 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.2433 mL | 16.2164 mL | 32.4328 mL | 81.0820 mL |
| 5 mM | 0.6487 mL | 3.2433 mL | 6.4866 mL | 16.2164 mL | |
| 10 mM | 0.3243 mL | 1.6216 mL | 3.2433 mL | 8.1082 mL | |
| 15 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL | 5.4055 mL | |
| 20 mM | 0.1622 mL | 0.8108 mL | 1.6216 mL | 4.0541 mL | |
| 25 mM | 0.1297 mL | 0.6487 mL | 1.2973 mL | 3.2433 mL | |
| 30 mM | 0.1081 mL | 0.5405 mL | 1.0811 mL | 2.7027 mL | |
| 40 mM | 0.0811 mL | 0.4054 mL | 0.8108 mL | 2.0270 mL | |
| 50 mM | 0.0649 mL | 0.3243 mL | 0.6487 mL | 1.6216 mL | |
| 60 mM | 0.0541 mL | 0.2703 mL | 0.5405 mL | 1.3514 mL | |
| 80 mM | 0.0405 mL | 0.2027 mL | 0.4054 mL | 1.0135 mL | |
| 100 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL |
(R)-(+)-Warfarin Related Classifications
HY-W015998 Related Classifications
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