| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
Betrixaban (trade name Bevyxxa; formerly PRT054021; MK-4448; PRT-021; MLN-1021 etc.) is a highly potent, selective, and orally bioavailalbe anticoagulant drug which acts as a direct factor Xa inhibitor. As of 2017, Betrixaban is approved by FDA for venous thrombosis prevention in adults hospitalized for an acute medical illness who are at risk for thromboembolic complications due to restricted mobility and other risk factors. Compared to other DOACs betrixaban has relatively low renal excretion (ca. 17%) and is not metabolized by CYP3A4.
| ln Vitro |
In patch clamp hERG tests, betrixaban (PRT054021) exhibits an IC50 of 8.9 μM[1]. Betrixaban exhibits an IC50 and a Ki for plasma kallikrein of 6.3 μM and 3.5 μM, respectively[1]. Compared to all other drugs (hERG Ki⩽0.5 μM), betrixaban (hERG Ki 1.8 μM) shows noticeably less hERG activity[1]. Betrixaban inhibits the production of thrombin (5–25 ng/mL)[3].
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| ln Vivo |
In dogs, betrixaban has an oral bioavailability of 51.6% (0.5 mg/kg, iv; 2.5 mg/kg, po)[1]. In monkeys, betrixaban has an oral bioavailability of 58.7% (0.75 mg/kg, iv; 7.5 mg/kg, po)[1]. R-Antidote reverses the whole-blood INR rise mediated by betrixaban. Following a 30-minute IV infusion, the overall plasma concentration of betrixaban is 0.2±0.01 μM, with 40%±7.2% of the inhibitor remaining unbound. Following r-Antidote delivery, the fraction of unbound inhibitor decreased to 0.3%±0.1% while the overall plasma concentration rose to 2.0±0.4 μM[2]. When used in the rabbit abdominal vena cava model of clot accretion on cotton threads, betrixaban (3 mg/kg) exhibits almost equal inhibition of thrombus mass to enoxaparin 1.6 mg/kg (76% vs. 96% inhibition)[3]. In the ferric chloride damage model of the rat carotid artery, betrixaban (19.1 mg/kg) is at least as effective as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d (90% vs. 70% vs. 80% patency, respectively) at maintaining patency[3].
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| Animal Protocol |
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| References |
[1]. Zhang P, et al. Discovery of Betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):21
[2]. Lu G, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51. [3]. Chan NC, et al. Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism. Vasc Health Risk Manag. 2015 Jun 26;11:343-51 |
| Molecular Formula |
C23H22CLN5O3
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|---|---|
| Molecular Weight |
451.91
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| CAS # |
330942-05-7
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| Related CAS # |
Betrixaban-d6;2098655-51-5;Betrixaban maleate;936539-80-9;Betrixaban hydrochloride;2099719-47-6
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| SMILES |
N=C(N(C)C)C(C=C1)=CC=C1C(NC2=CC=C(OC)C=C2C(NC(C=C3)=NC=C3Cl)=O)=O
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| Chemical Name |
N-(5-Chloropyridin-2-yl)-2-((4-(N,N-dimethylcarbamimidoyl)benzoyl)amino)-5- methoxybenzamide
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| Synonyms |
PRT054021; PRT-021; MK-4448; MLN-1021; PRT 054021; PRT-054021; MK4448; MLN 1021; PRT 021; PRT021; MK 4448; MLN1021; trade name Bevyxxa
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2128 mL | 11.0641 mL | 22.1283 mL | |
| 5 mM | 0.4426 mL | 2.2128 mL | 4.4257 mL | |
| 10 mM | 0.2213 mL | 1.1064 mL | 2.2128 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.
(a) Dose-dependent reversal of betrixaban, rivaroxaban and apixaban inhibition in fXa enzyme assays. (b) Reversal of the prolongation of prothrombin time (PT) produced by rivaroxaban in human plasma after incubation of rivaroxaban (1 μM) with different concentrations of r-Antidote at room temperature for 30 min before initiation of the assay.Nat Med.2013 Apr;19(4):446-51. |
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(a) Whole-blood INR values (mean ± s.d.) in rats infused with rivaroxaban (0.25 mg per kg body weight h−1) or vehicle for 30 min and then treated with either vehicle or r-Antidote by i.v. bolus (4 mg) over 5 min plus infusion (4 mg h−1) for up to 90 min. (b) Whole-blood INR values (mean ± s.d.) in rats infused with betrixaban (1 mg per kg body weight h−1) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6 mg) over 5 min plus infusion (9 mg h−1) for up to 90 min.Nat Med.2013 Apr;19(4):446-51. |
a) Dose titration of r-Antidote for the mitigation of blood loss caused by enoxaparin-induced anticoagulation in the indicated groups. (b) Mitigation of blood loss caused by fondaparinux-induced anticoagulation with r-Antidote in the indicated groups. Treat-I, vehicle treatment alone;(c) The anti-fXa activity in fondaparinux-anticoagulated rats (shown inb) at different time points for the Treat-II (square), Treat-III (diamond) and Treat-IV (inverted triangle) groups.Nat Med.2013 Apr;19(4):446-51. |
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