Name | Edoxaban (tosylate Monohydrate) |
Synonyms | Edoxaban tosilate edoxaban tosylate hydrate Edoxaban Tosylate Hydrate 1 Edoxaban (tosylate Monohydrate) Edoxaban p-toluenesulfonate monohydrate N1-(5-Chloropyridin-2-yl)-N2-((1S,2R,4S)-4-(dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)cyclohexyl)oxalamide 4-methylbenzenesulfonate hydrate N-(5-Chloropyridin-2-yl)-N'-((1S,2R,4S)-4-[(dimethyl amino)carbonyl]-2-[[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl)ethanediamide p-toluenesulfonate monohydrate Ethanediamide, N1-(5-chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]-, 4-methylbenzenesulfonate, hydrate |
CAS | 1229194-11-9 |
EINECS | 1592732-453-0 |
Molecular Formula | C31H38ClN7O7S2 |
Molar Mass | 720.26 |
Melting Point | >252°C (dec.) |
Solubility | 10 mM in DMSO |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
Physical and Chemical Properties | Bioactive Edoxaban (DU-176b) is a selective inhibitor of factor Xa and an anticoagulant with oral effect. |
In vitro study | In human plasma, Edoxaban at 0.256 and 0.508 μm, respectively, doubled the prothrombin time and activated the partial thromboplastin time. |
In vivo study | Oral administration of Edoxaban resulted in potent anti-Xa activity and high plasma drug concentrations in rats and monkeys. In in vivo experiments, Edoxaban dose-dependently inhibited thrombosis in rat and rabbit thrombosis models. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.355 ml | 6.773 ml | 13.545 ml |
5 mM | 0.271 ml | 1.355 ml | 2.709 ml |
10 mM | 0.135 ml | 0.677 ml | 1.355 ml |
5 mM | 0.027 ml | 0.135 ml | 0.271 ml |
in vitro study |
In human plasma, 0.256 and 0.508 μM Edoxaban double the prothrombin time and activate part of the prothrombin kinase time. |
in vivo study | In rats and monkeys, Edoxaban oral administration produces effective anti-Xa activity and high plasma drug concentration. In vivo experiments, Edoxaban dose-dependent inhibition of thrombosis in rat and rabbit models of thrombosis. |
anticoagulants | On January 8, 2015, the US FDA approved the anticoagulant drug Idusaban (Edoxaban) of Daiichi Sankyo Pharmaceutical Company of Japan, with the trade name Savaysa. Idusaban is a selective coagulation factor Xa inhibitor oral tablet for the prevention and treatment of deep vein thrombosis and pulmonary embolism. It is used to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (NVAF). There are currently three specifications: 60mg, 30mg and 15 mg. | ||||
biological activity | Edoxaban (DU-176b) is a selective inhibitor of factor Xa and an anticoagulant with oral effect. | ||||
Target |
|
anticoagulant | On January 8, 2015, the US FDA approved the anticoagulant drug Idusaban (Edoxaban) of Japan's Sankyo Pharmaceutical Company (Daiichi Sankyo), with the trade name Savaysa. Idusaban is a selective coagulation factor Xa inhibitor oral tablet for the prevention and treatment of deep vein thrombosis and pulmonary embolism. It is used to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (NVAF). There are currently three specifications: 60mg, 30mg and 15 mg. |
biological activity | Edoxaban (DU-176b) is a factor Xa selective inhibitor and an anticoagulant with oral effect. |
target | TargetValue Factor Xa (Cell-free say) 0.561 nM(Ki) |
Target | Value |
Factor Xa (Cell-free assay) | 0.561 nM(Ki) |
In vitro study | In human plasma, 0.256 and 0.508 μM Edoxaban double prothrombin time and activate partial thromboplastin time. |
in vivo studies | in rats and monkeys, Edoxaban oral administration produces effective anti-Xa activity and high plasma drug concentration. In vivo experiments Edoxaban dose-dependent inhibition of thrombosis in rat and rabbit models of thrombosis. |