Darexaban
Modify Date: 2024-01-09 17:48:13
Darexaban structure
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Common Name | Darexaban | ||
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| CAS Number | 365462-23-3 | Molecular Weight | 474.55 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C27H30N4O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of DarexabanDarexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects[1][2][3]. |
| Name | N-[2-hydroxy-6-[(4-methoxybenzoyl)amino]phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide |
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| Synonym | More Synonyms |
| Description | Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects[1][2][3]. |
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| Related Catalog | |
| In Vitro | Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa[2]. |
| In Vivo | In mice, Darexaban inhibits FXa activity in plasma with an ED50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg[2]. In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg[2]. In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher[2]. |
| References |
| Molecular Formula | C27H30N4O4 |
|---|---|
| Molecular Weight | 474.55 |
| Exact Mass | 474.22700 |
| PSA | 94.14000 |
| LogP | 4.19620 |
| Hazard Codes | Xi |
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Darexaban CAS#:365462-23-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 54, # 23 p. 8051 - 8065 |
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Darexaban CAS#:365462-23-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 54, # 23 p. 8051 - 8065 |
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Darexaban CAS#:365462-23-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 54, # 23 p. 8051 - 8065 |
|
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Darexaban CAS#:365462-23-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 54, # 23 p. 8051 - 8065 |
| Precursor 3 | |
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| DownStream 0 | |
| Darexaban |
| UNII-KF322K101S |
| Tanexaban |