| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Zifaxaban targets Factor Xa (FXa), a key enzyme in the coagulation cascade that converts prothrombin to thrombin. It is a competitive and selective inhibitor of FXa with an IC50 of 11.1 nM for human FXa. Zifaxaban is more than 10,000 times more selective for FXa than other serine proteases.
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|---|---|
| ln Vitro |
Zifaxaban is a potent inhibitor of Factor Xa with an IC50 of 11.1 nM. It is highly selective for FXa, with more than 10,000-fold selectivity over other serine proteases. The compound is orally active and competitive. Zifaxaban inhibits thrombus formation in a dose-dependent manner.
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| ln Vivo |
Zifaxaban produced a severe vascular embolism in the arterial vascular shunt model, with an ED50 value of 3.09 mg/kg, and its optimal lesion time happened after two hours [1]. In a model of thrombosis, Zifaxaban inhibits thrombosis in a dose-dependent way [1].
Zifaxaban inhibits thrombus formation in a dose-dependent manner in rat arteriovenous shunt thrombosis and carotid artery thrombosis models. As an orally active FXa inhibitor, it is expected to exhibit antithrombotic efficacy in preclinical models of arterial and venous thrombosis. Further research is needed to fully characterize its pharmacokinetic and pharmacodynamic profiles. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for Zifaxaban typically involves measuring its inhibitory activity against Factor Xa using a standard chromogenic or fluorogenic substrate assay. The compound is incubated with FXa and a substrate, and the enzymatic activity is measured. The IC50 value is determined from the dose-response curve.
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| Cell Assay |
The in vitro cellular assay for Zifaxaban typically involves culturing relevant cell types or using plasma samples to assess its effects on coagulation. The compound is tested at various concentrations, and its ability to inhibit FXa activity and prolong clotting times is measured using standard coagulation assays such as prothrombin time (PT) or activated partial thromboplastin time (aPTT).
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| Animal Protocol |
In vivo animal studies for Zifaxaban typically involve the use of rat models of thrombosis, such as the arteriovenous shunt thrombosis model or the carotid artery thrombosis model. Animals are administered the compound via oral gavage at various doses, and thrombus formation is assessed. The compound's antithrombotic efficacy and effects on bleeding time are evaluated.
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| ADME/Pharmacokinetics |
Zifaxaban has a molecular weight of 429.88 g/mol and a molecular formula of C20H16ClN3O4S. The IUPAC name is 5-chloro-N-[[(5R)-2-oxo-3-[4-(2-oxopyridin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide. The compound is also known as TY-602. Further detailed physicochemical properties are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Specific toxicology data for Zifaxaban are not available in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. As an anticoagulant, it may increase the risk of bleeding. Standard safety assessments would be required before any clinical application.
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| References | |
| Additional Infomation |
Zifaxaban (TY-602) is an orally active, competitive, and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. It is more than 10,000 times more selective for FXa than other serine proteases. Zifaxaban can be used for the study of arterial and venous thrombosis. It has not yet entered clinical trials and is strictly for preclinical research purposes.
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| Molecular Formula |
C20H16CLN3O4S
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|---|---|
| Molecular Weight |
429.875
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| Exact Mass |
429.054
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| CAS # |
1378266-98-8
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| PubChem CID |
60172452
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
680.2±55.0 °C at 760 mmHg
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| Flash Point |
365.2±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
2.45
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
723
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=CC=C(C(NC[C@H]2CN(C(=O)O2)C2C=CC(=CC=2)N2C=CC=CC2=O)=O)S1
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| InChi Key |
MXWOUAQNXIUJIN-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C20H16ClN3O4S/c21-17-9-8-16(29-17)19(26)22-11-15-12-24(20(27)28-15)14-6-4-13(5-7-14)23-10-2-1-3-18(23)25/h1-10,15H,11-12H2,(H,22,26)/t15-/m0/s1
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| Chemical Name |
5-chloro-N-[[(5S)-2-oxo-3-[4-(2-oxopyridin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
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| Synonyms |
TY 602; TY602; TY-602
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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) |
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
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| 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 | 2.3262 mL | 11.6312 mL | 23.2623 mL | |
| 5 mM | 0.4652 mL | 2.3262 mL | 4.6525 mL | |
| 10 mM | 0.2326 mL | 1.1631 mL | 2.3262 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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