Edoxaban
Edoxaban
CAS: 480449-70-5;912273-65-5
Molecular Formula: C24H30ClN7O4S
Edoxaban - Names and Identifiers
Edoxaban - Physico-chemical Properties
| Molecular Formula | C24H30ClN7O4S |
| Molar Mass | 548.06 |
| Density | 1.43 |
| Melting Point | >213°C (dec.) |
| Solubility | 25°C: DMSO |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 9.46±0.70(Predicted) |
| Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
Edoxaban - Introduction
Edoxaban(DU-176) is an oral FXa inhibitor, clinically developed for stroke prevention.
Last Update：2022-10-16 17:25:23
Edoxaban - Reference Information
| LogP | -1.455 |
| introduction | edoxaban, chemical name: N-(5-chloropyridine-2-yl)-N'-((1S,2R,4S)-4-[(dimethylamino) carbonyl]-2-{[(5-methyl -4,5,6, 7-tetrahydrothiazolo [5,4-c] pyridine-2-yl) carbonyl] amino} cyclohexyl) ethanediamide, toluene sulfonate is used in the preparation. It is a small molecule oral anticoagulant developed by Japan's Daiichi Sankyo Co., Ltd. and is a coagulation factor X(FXa) inhibitor. During the coagulation process, activated coagulation factor X(FXa) activates prothrombin (FII) into thrombin (FIIa), which promotes the formation of fibrin and thus forms thrombus. Therefore, FXa has become the main target for the development of a new generation of anticoagulant drugs. |
| pharmacological action | edoxaban is a reversible factor Xa inhibitor with high selectivity and can directly inhibit FXa. as a result, prothrombin time (prothrombintime,PT) and activated partial thromboplastin time (activatedpartialthromboplastintime,APTT) can be prolonged, and finally thrombosis can be inhibited. Due to the amplification of biological signals in the coagulation process, a factor Xa inhibitor molecule can inhibit the physiological effect of 138 prothrombin molecules. Therefore, factor Xa inhibitor is more effective than thrombin inhibitor. The therapeutic dose of edoxaban has an effect on PT, international normalized ratio (internationalnormalizedratio,INR) and APTT, but the change is small. Peak concentration (Cmax) can be reached 1~2 hours after oral administration. |
| preparation | at room temperature, to N-(5-chloropiperidine-2-yl)-N'-[(1S,2R,4S)-4-(N, methanesulfonic acid (66ml) was added to the suspension of acetonitrile (1900ml) of N-dimethylformylamino)-2-(aminotera-butoxycarbonyl) cyclohexyl] oxamide (95.1g) and stirred at this temperature for 2 hours. Under ice cold, triethylamine (155ml), 4,5,6,7-tetrahydro-5-methyl-thiazolo [5,4-c] pyridine-2-carboxylic acid hydrochloride (52.5g), 1-hydroxybenzotriazole (33.0g), 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (46.8g) were added to the reaction solution, stir at room temperature for 16 hours. Add triethylamine and water, and stir for 1 hour under ice cold, then filter out crystals to obtain compound (1), namely 103.2g of eidoxaban. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 20:49:11
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