Edoxaban (tosylate)

Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively). It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.Formal Name: 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, ethanediamide. CAS Number: 480449-71-6. Synonyms: DU-176b. Molecular Formula: C24H30ClN7O4S . C7H8O3S. Formula Weight: 720.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: ClC1=CN=C(NC(C(N[C@H]2CC[C@H](C(N(C)C)=O)C[C@H]2NC(C3=NC4=C(CN(C)CC4)S3)=O)=O)=O)C=C1.CC5=CC=C(S(O)(=O)=O)C=C5. InChi Code: InChI=1S/C24H30ClN7O4S.C7H8O3S/c1-31(2)24(36)13-4-6-15(27-20(33)21(34)30-19-7-5-14(25)11-26-19)17(10-13)28-22(35)23-29-16-8-9-32(3)12-18(16)37-23,1-6-2-4-7(5-3-6)11(8,9)10/h5,7,11,13,15,17H,4,6,8-10,12H2,1-3H3,(H,27,33)(H,28,35)(H,26,30,34),2-5H,1H3,(H,8,9,10)/t13-,15-,17+,/m0./s1. InChi Key: ZLFZITWZOYXXAW-QXXZOGQOSA-N.