936539-80-9
936539-80-9 structure
- Name: Betrixaban maleate
- Chemical Name: N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide maleate
- CAS Number: 936539-80-9
- Molecular Formula: C27H26ClN5O7
- Molecular Weight: 567.97800
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Factor Xa
- Create Date: 2018-10-17 11:26:45
- Modify Date: 2024-01-12 09:17:39
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Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect[1][3].
| Name | N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide maleate |
|---|---|
| Synonyms | Betrixaban maleate |
| Description | Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect[1][3]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 1.5 nM (fXa)[1] Ki: 0.117 nM (fXa), 1.8 μM (hERG)[1] |
| In Vitro | Betrixaban (PRT054021) shows IC50 of 8.9 μM in patch clamp hERG assays[1]. Betrixaban shows an IC50 and a Ki of 6.3 μM and 3.5 μM for the plasma kallikrein, respectively[1]. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽0.5 μM)[1]. Betrixaban (5-25 ng/mL) inhibits thrombin generation[3]. |
| In Vivo | Betrixaban (0.5 mg/kg, i.v.; 2.5 mg/kg, p.o.) has bioavailability of 51.6% in dog[1]. Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has bioavailability of 58.7% in monkey[1]. Betrixaban mediated whole-blood INR increase is reversed by r-Antidote. After i.v. infusion for 30 min, the total plasma concentrations of Betrixaban is 0.2±0.01 μM, and the percentages of unbound inhibitor is 40%±7.2%. After administration of r-Antidote, the total plasma concentration increased to 2.0±0.4 μM, and the percentage of unbound inhibitor declined to 0.3%±0.1%[2]. Betrixaban (3 mg/kg) shows nearly comparable inhibition of thrombus mass to enoxaparin 1.6 mg/kg (76% vs 96% inhibition) in the rabbit abdominal vena cava model of clot accretion on cotton threads[3]. Betrixaban (19.1 mg/kg) is at least as effective at maintaining patency as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d (90% vs 70% vs 80% patency, respectively) in the ferric chloride injury model of rodent carotid artery[3]. |
| References |
| Molecular Formula | C27H26ClN5O7 |
|---|---|
| Molecular Weight | 567.97800 |
| Exact Mass | 567.15200 |
| PSA | 182.01000 |
| LogP | 4.09270 |
| Storage condition | 2-8℃ |