N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺
Betrixaban
CAS: 330942-05-7
Molecular Formula: C23H22ClN5O3
N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺 - Names and Identifiers
N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺 - Physico-chemical Properties
| Molecular Formula | C23H22ClN5O3 |
| Molar Mass | 451.91 |
| Density | 1.30±0.1 g/cm3(Predicted) |
| Melting Point | 210-213°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Off-White |
| pKa | 11.00±0.70(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | In patch clamp hERG assays, Betrixaban has IC 50 of 8.9 μM. The plasma kallikrein IC 50 and K i values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG K i 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG K i ⩽0.5 μM). |
| In vivo study | Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey. Both Betrixaban and Apixa-ban-mediated whole-blood INR increases are similarly reversed by r-Antidote. After i.v. infusion of the three fXa inhibitors (each admin¬istered individually) for 30 min, the total plasma concentrations of rivaroxaban, Betrixaban and apixaban are 1.4±0.4 μM (mean±s.d.), 0.2±0.01 μM and 1.4±0.3 μM, respectively, and the percentages of unbound inhibitor are 2.2%±0.8% (mean±s.d.), 40%±7.2% and 1.5%±0.3%, respectively. After administration of r-Antidote, the total plasma concentrations of the inhibitors increased to 1.9±0.09 μM, 2.0±0.4 μM and 4.2±0.7 μM, respectively, and the percentage of unbound inhibitor declined to 0%, 0.3%±0.1% and 0.05%±0.02%, respectively. Thus, for each of the three inhibitors, correction of prothrombin time by r-Antidote to near-normal values is associated with a reduction in the free fraction of the inhibitor. |
N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.213 ml | 11.064 ml | 22.128 ml |
| 5 mM | 0.443 ml | 2.213 ml | 4.426 ml |
| 10 mM | 0.221 ml | 1.106 ml | 2.213 ml |
| 5 mM | 0.044 ml | 0.221 ml | 0.443 ml |
Last Update：2024-01-02 23:10:35
N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺 - Reference Information
| Use | Betrixiban (Betrixiban) is a new, selective, directly acting on factor Xa, effective oral anticoagulants with potential to prevent post-knee embolism and post-stroke atrial tremor are currently in Phase III clinical trials, the role of betrixaban in patients at high risk for venous thromboembolism is being evaluated in a global Phase III trial. It was developed by Portola Pharmaceuticals and developed in collaboration with Merck in the United States for clinical research in 2009, the clinical study phase was conducted by Portora pharmaceutical company alone. Compared with the already marketed serine protease factor Xa inhibitor, betrixaban has the characteristic of being not metabolized by cytochrome P450 3A4(CYP3A4), which reduces the risk of drug-drug interaction. Data from a Phase II clinical trial of betrixaban showed similar efficacy and safety to low-molecular-weight heparin. Betrixaban is excreted by bile, so patients with thrombosis with renal insufficiency can benefit from it. In an exploratory clinical trial of betrixaban in the United States and Canada, 215 patients after hip surgery were randomized 2 : 2 : 1 to the 15 mg, 40 mg betrixaban group (dose blinded). And enoxaparin 30 mg group, the results of venous embolization of betrosiban 15 mg group was 20%, 40 mg group was 15%, enoxaparin group was 10%, 2.4% of clinically significant non-major bleeding in the 40 mg betroxiban group, 2.3% of major bleeding in the enoxaparin group, and 4.6% of clinically significant non-major bleeding, indicating a dose-dependent efficacy of betroxiban, and better tolerated than enoxaparin. |
| background significance | Heparin, low molecular weight heparin, warfarin and other traditional anticoagulant drugs, there are certain limitations in the use, for example, unfractionated heparin needs to be regularly monitored by activated partial thromboplastin time (APTT); Low molecular weight heparin is an intravenous preparation; Warfarin needs frequent monitoring because of its slow onset, its international normalized ratio (INR) is easy to fluctuate and can not be predicted, easy to interact with other drugs or food, and the dose needs to be individualized and other shortcomings, these shortcomings greatly limit the use of traditional anticoagulant drugs in clinical applications. In recent years, the study of new anticoagulant drugs has become a hot spot in clinical research. Betrixaban has broad application prospects and is an anticoagulant drug worthy of attention and research by researchers, so it has research value. |
| biological activity | Betrixaban (PRT054021) is a potent, orally active selective factor Xa (fXa) inhibitor, IC50 1.5 nM. |
| Target | TargetValue Factor Xa (Cell-free assay) 1.5 nM |
| Target | Value |
| Factor Xa (Cell-free assay) | 1.5 nM |
| In vitro study | In patch clamp hERG populations, Betrixaban has IC 50 of 8.9 μm. The plasma kallikelin IC 50 and K I values for Betrixaban are 6.3 μm and 3.5 μm review. (hERG K I 1.8 μm). |
| in vivo study | Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, betrixaban has bio-availability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bio-availability of 58.7% in monkey. All Apixa-ban-mediated whole-blood INR increases are numerically reversed by r-Antidote. After I. v. infusion of the three fXa inhibitors (each admin¬istered individually) for 30 min, the total plasma concentrations of rivaroxaban, Betrixaban and apixaban are 1.4±0.4 μM (mean±s.d.), 0.2±0.01 μM and 1.4±0.3 μM, respectively, and the percentages of unbound inhibitor are 2.2%±0.8% (mean±s.d.), 40%±7.2% and 1.5%±0.3%, respectively. After administration of r-Antidote the total plasma concentrations of the inhibitors increased to 1.9±0.09 μM, 2.0±0.4 μM and 4.2±0.7 μM, respectively, and the percentage of unbound inhibitor declined to 0%, 0.3%±0.1% and 0.05%±0.02% respectively. Thus, for each of the three inhibitors, correction of prothrombin time by r-Antidote to near-normal values is associated with a reduction in the free fraction of the inhibitor. |
Last Update：2024-04-09 21:54:55
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View History
N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺
Boronic acid, B-[3-chloro-4,5-bis(1-methylethoxy)phenyl]-
N-(4,5-二甲基-1H-咪唑-2-基)乙酰胺
2-(Di-1-adaMantylphosphino)-3,6-diMethoxy-2',4',6'-tri-i-propyl-1,1'-biphenyl
(6-chloro-4,5-dimethyl-3-pyridazinyl)-2-pyridinyl-Methanone
1-(Ethylamino)cyclohexanecarbonitrile
Glycine, N-[N-[1-(methoxycarbonyl)-2-methylpropyl]-L-valyl]-, ethyl ester, (S)- (9CI)
埃索美拉唑杂质L
(4-溴苯基)三甲基硅烷
磺胺二甲氧嘧啶杂质C (EP)
Boronic acid, B-[3-chloro-4,5-bis(1-methylethoxy)phenyl]-
N-(4,5-二甲基-1H-咪唑-2-基)乙酰胺
2-(Di-1-adaMantylphosphino)-3,6-diMethoxy-2',4',6'-tri-i-propyl-1,1'-biphenyl
(6-chloro-4,5-dimethyl-3-pyridazinyl)-2-pyridinyl-Methanone
1-(Ethylamino)cyclohexanecarbonitrile
Glycine, N-[N-[1-(methoxycarbonyl)-2-methylpropyl]-L-valyl]-, ethyl ester, (S)- (9CI)
埃索美拉唑杂质L
(4-溴苯基)三甲基硅烷
磺胺二甲氧嘧啶杂质C (EP)