Imvelaphi

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, inamandla amancinci-imolekyuli inhibitor ye-factor Xa eyi-coagulation factor ngexesha elibalulekileyo kwi-coagulation pathway yegazi ekhokelela kwisizukulwana. i-thrombin kunye nokwakheka kwehlwili. I-Rivaroxaban ibophelela kwi-Tyr288 kwi-pocket ye-S1 ye-factor Xa ngokusebenzisa i-Tyr288 kunye ne-chlorine substituent ye-chlorothiophene moiety. I-inhibition iguqulwa (koff = 5x10-3s-1), ngokukhawuleza (kon = 1.7x107 mol / L-1 s-1), kunye nokuxhomekeka koxinzelelo (Ki = 0.4 nmol / L). I-Rivaroxaban okwangoku ifundelwa unyango lwe-VTE, ukuthintela iziganeko ze-cardiovascular kwizigulane ezine-acute coronary syndrome, ukuthintela ukubetha kwizigulane ezine-fibrillation ye-atrial.

Isalathiso

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, kunye noVolker Laux. I-Rivaroxaban: i-oral factor Xa inhibitor entsha. I-Arterioscler Thromb Vasc Biol 2010; 30(3): 376-381

Inkcazo

I-Rivaroxaban (i-BAY 59-7939) inamandla kakhulu,i-Factor Xa (FXa) inhibitor ekhethiweyo kunye nethe ngqo, ukuphumeza inzuzo enamandla kwi-anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

I-In vitro

I-Rivaroxaban (i-BAY 59-7939) yi-inhibitor yomlomo, ngokuthe ngqo kwi-Factor Xa (FXa) ekuphuhliseni ukuthintela kunye nokunyangwa kwe-arterial and venous thrombosis. I-Rivaroxaban inqanda ngokukhuphisanayo i-FXa yomntu (i-Ki 0.4 nM) kunye > i-10 000-fold selectivity enkulu kunezinye i-serine proteases; kwakhona inqanda umsebenzi weprothrombinase (IC50 2.1 nM). I-Rivaroxaban inqanda i-endogenous FXa inamandla ngakumbi kwi-plasma yomntu kunye nomvundla (IC50 21 nM) kune-rat plasma (IC50 290 nM). Ibonisa imiphumo ye-anticoagulant kwi-plasma yomntu, ixesha eliphindwe kabini le-prothrombin (PT) kwaye lisebenzise ixesha le-thromboplastin inxalenye kwi-0.23 kunye ne-0.69μM, ngokulandelelanayo.

I-Rivaroxaban (i-BAY 59-7939) inamandla kwaye ikhethayo, i-FXa inhibitor echanekileyo kunye ne-extreme in vivo kunye ne-bioavailability yomlomo. I-Rivaroxaban (BAY 59-7939), elawulwa yi-iv bolus ngaphambi kokungeniswa kwe-thrombus, iyanciphisa ukubunjwa kwe-thrombus (ED50 0.1 mg / kg), inqanda i-FXa, kwaye yandisa umthamo we-PT ngokuxhomekeka. I-PT kunye ne-FXa zichaphazeleka kancinci kwi-ED50 (ukwanda kwe-1.8-fold kunye ne-32% inhibition, ngokulandelanayo). Kwi-0.3 mg / kg (i-dose ekhokelela ekuthinteleni phantse ngokupheleleyo ukubunjwa kwe-thrombus), i-Rivaroxaban imodareyitha i-PT (3.2)±I-0.5-fold) kwaye inqanda umsebenzi we-FXa (65±3%).

Ugcino

Ubume beMichiza