| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Betrixaban maleate targets factor Xa (fXa), a key enzyme in the coagulation cascade. Factor Xa converts prothrombin to thrombin, which is essential for the formation of fibrin clots. By inhibiting fXa, Betrixaban decreases prothrombinase activity and thrombin generation, thereby preventing thrombus formation. This mechanism underlies its antithrombotic effects.
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| ln Vitro |
In a patch-clamp hERG test, betrixaban (PRT054021) has an IC50 of 8.9 μM [1]. Betrixaban's IC50 and Ki against plasma kallikrein are 6.3 μM and 3.5 μM, respectively [1]. Compared to all other medications (hERG Ki ⩽0.5 μM), betrixaban (hERG Ki 1.8 μM) exhibits noticeably decreased hERG activity [1]. Betrixaban (5-25 ng/mL) prevents the synthesis of thrombin [3].
In vitro, Betrixaban maleate is a potent inhibitor of factor Xa with an IC50 of 1.5 nM. This demonstrates its high potency as a fXa inhibitor. Its activity is characterized in cell-free enzymatic assays measuring the inhibition of fXa activity. |
| ln Vivo |
The oral bioavailability of betrixaban (0.5 mg/kg intravenously; 2.5 mg/kg orally) in dogs is 51.6% [1]. The oral bioavailability of betrixaban (0.75 mg/kg intravenously; 7.5 mg/kg orally) in monkeys is 58.7% [1]. Betrixaban-mediated rise of whole blood INR was reversed by r-Antidote. After 30 minutes of intravenous administration, the overall plasma concentration of betrixaban was 0.2 ± 0.01 μM, and the fraction of unbound inhibitor was 40% ± 7.2%. After delivery of r-Antidote, total plasma concentration increased to 2.0±0.4 μM and the fraction of unbound inhibitor fell to 0.3%±0.1%[2]. In the rabbit intraperitoneal vein model of clot accumulation on cotton threads, the inhibition of thrombus mass by betrixaban (3 mg/kg) was practically equal to that of enoxaparin 1.6 mg/kg (76% vs. 96% inhibition) [3 ]. In a mouse model of ferric chloride damage, betrixaban (19.1 mg/kg) was at least as effective as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d in maintaining patency (patency rates, respectively 90% vs 70% vs 80%) carotid artery [3].
In vivo, Betrixaban maleate is used clinically as an antithrombotic agent to prevent venous thromboembolism in high-risk hospitalized patients. It is an orally active compound, making it suitable for oral administration. Its efficacy in reducing the risk of deep vein thrombosis and pulmonary embolus has been established in clinical trials. |
| Enzyme Assay |
A cell-free assay for Betrixaban maleate involves measuring its inhibition of factor Xa enzymatic activity. In this assay, recombinant fXa is incubated with a chromogenic or fluorogenic substrate in the presence of varying concentrations of the compound. The rate of substrate cleavage is measured, and the IC50 is calculated. For Betrixaban, the IC50 is 1.5 nM.
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| Cell Assay |
Cellular assays for Betrixaban maleate are not typically performed, as its target is a soluble enzyme in the coagulation cascade. Its activity is assessed in plasma-based assays measuring clotting time or thrombin generation. Specific protocols are not detailed.
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| Animal Protocol |
In vivo animal experiments for Betrixaban maleate are not described in the available sources. As a clinically used drug, its efficacy and safety have been established in human studies. Preclinical studies in animal models of thrombosis likely contributed to its development, but specific protocols and data are not provided.
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| ADME/Pharmacokinetics |
Betrixaban maleate is an orally active compound. Specific pharmacokinetic parameters, such as half-life, bioavailability, and metabolism, are not provided in the available sources. As an antithrombotic agent, it is designed for oral administration.
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| Toxicity/Toxicokinetics |
Toxicity data for Betrixaban maleate are not detailed in the available sources. As an FDA-approved drug, its safety profile is established. Common adverse effects include bleeding, which is a risk associated with all anticoagulants. Specific toxicological information is not provided.
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| References |
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| Additional Infomation |
See also: Betrixaban (Note moved to).
Betrixaban maleate (CAS: 936539-80-9) is a potent, orally active, selective factor Xa inhibitor. It is also known as PRT054021 maleate. It has an IC50 of 1.5 nM for fXa and has antithrombotic effects. It is used to decrease the risk of deep vein thrombosis and pulmonary embolus in hospitalized patients at high risk for venous thromboses. Its molecular formula is C27H26ClN5O7. |
| Molecular Formula |
C27H26CLN5O7
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|---|---|
| Molecular Weight |
568.0
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| Exact Mass |
567.152
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| CAS # |
936539-80-9
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| Related CAS # |
Betrixaban;330942-05-7;Betrixaban hydrochloride;2099719-47-6
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| PubChem CID |
16069304
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.092
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
40
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| Complexity |
787
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C(=O)O)=C/C(=O)O.N(C1=CC=C(OC)C=C1C(=O)NC1N=CC(Cl)=CC=1)C(C1C=CC(C(=N)N(C)C)=CC=1)=O
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| InChi Key |
DTSJEZCXVWQKCL-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C23H22ClN5O3.C4H4O4/c1-29(2)21(25)14-4-6-15(7-5-14)22(30)27-19-10-9-17(32-3)12-18(19)23(31)28-20-11-8-16(24)13-26-20;5-3(6)1-2-4(7)8/h4-13,25H,1-3H3,(H,27,30)(H,26,28,31);1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
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| Synonyms |
PRT-054021; betrixaban maleate; PRT 054021; PRT054021; 936539-80-9; Betrixaban maleate [WHO-DD]; 28Z3021TMU; BETRIXABAN MALEATE [MI];
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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 | 1.7606 mL | 8.8028 mL | 17.6056 mL | |
| 5 mM | 0.3521 mL | 1.7606 mL | 3.5211 mL | |
| 10 mM | 0.1761 mL | 0.8803 mL | 1.7606 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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