Rivaroxaban
ndabere
Rivaroxaban, 5-chloro-N-[[(5S) -2-oxo-3-[4- (3-oxomorpholin-4-yl) phenyl]-1,3-oxazolidin-5-yl]methyl] thiophene-2 -carboxamide, bụ ihe na-eme ka obere molecule na-egbochi ihe Xa nke bụ ihe na-akpata coagulation n'oge dị oké egwu n'okporo ụzọ coagulation ọbara na-akpata ọgbọ nke thrombin na nhazi nke clot.Rivaroxaban na-ejikọta na Tyr288 na S1 akpa ego nke Xa site na mmekọrịta nke Tyr288 na chlorine n'ime chlorothiophene moiety.Mgbochi a na-agbanwe agbanwe (koff = 5x10-3s-1), ngwa ngwa (kon = 1.7x107 mol / L-1 s-1), na n'ụzọ dabere na ntinye uche (Ki = 0.4 nmol / L).A na-amụ Rivaroxaban ugbu a maka ọgwụgwọ VTE, mgbochi nke ọrịa obi na ndị ọrịa nwere nnukwu ọrịa obi, mgbochi nke ọrịa strok na ndị ọrịa nwere fibrillation atrial.
Ntụaka
Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, na Volker Laux.Rivaroxaban: ihe mgbochi ọnụ ọhụrụ Xa.Arterioscler Thromb Vasc Biol 2010;30 (3): 376-381
Nkọwa
Rivaroxaban (BAY 59-7939) bụ ike dị ukwuu,onye na-emechi ihe na-eme ihe na-ahụ maka Xa (FXa), na-enweta uru siri ike na ike mgbochi FXa (IC50 0.7 nM; Ki 0.4 nM).
Na Vitro
Rivaroxaban (BAY 59-7939) bụ onye na-emechi ọnụ, kpọmkwem Factor Xa (FXa) inhibitor na mmepe maka mgbochi na ọgwụgwọ nke arterial na venous thrombosis.Rivaroxaban asọmpi na-egbochi mmadụ FXa (Ki 0.4 nM) na> 10 000-fold nhọrọ ukwuu karịa maka proteases serine ndị ọzọ;ọ na-egbochikwa ọrụ prothrombinase (IC50 2.1 nM).Rivaroxaban na-egbochi FXa endogenous nke ọma na plasma mmadụ na oke bekee (IC50 21 nM) karịa plasma oke (IC50 290 nM).Ọ na-egosiputa mmetụta anticoagulant na plasma mmadụ, na-abawanye oge prothrombin ugboro abụọ (PT) ma na-arụ ọrụ thromboplastin akụkụ na 0.23 na 0.69.μM, n'otu n'otu.
Rivaroxaban (BAY 59-7939) bụ onye nwere ike na nhọrọ, onye na-egbochi FXa kpọmkwem nwere ọmarịcha ọrụ vivo yana ezigbo bioavailability ọnụ.Rivaroxaban (BAY 59-7939), nke iv bolus na-elekọta tupu mmalite thrombus, na-ebelata nhazi thrombus (ED50 0.1 mg/kg), na-egbochi FXa, ma na-agbatị dose PT dabere.PT na FXa na-emetụta ntakịrị na ED50 (mmụba okpukpu 1.8 na mgbochi 32%, n'otu n'otu).Na 0.3 mg / kg (ọgwụ nke na-eduga na njedebe zuru oke nke mmepụta thrombus), Rivaroxaban na-agbatị PT (3.2) ogologo oge.±0.5-fold) ma gbochie ọrụ FXa (65±3%).
Nchekwa
| Ntụ ntụ | -20°C | Afọ 3 |
| 4°C | afọ 2 | |
| Na ihe mgbaze | -80 Celsius | Ọnwa isii |
| -20°C | 1 ọnwa |
Ọdịdị chemical
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