Ka hope

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 ʻO -carboxamide, he mea hoʻopaneʻe liʻiliʻi liʻiliʻi o ka factor Xa kahi mea coagulation ma kahi manawa koʻikoʻi i ke ala coagulation koko e hopena i ka hana o ka thrombin a me ka hoʻokumu ʻana o ka clot.Hoʻopaʻa ʻo Rivaroxaban i ka Tyr288 ma ka ʻeke S1 o ka helu Xa ma o ka launa pū ʻana o Tyr288 a me ka chlorine substituent o ka chlorothiophene moiety.Hiki ke hoʻohuli ʻia ka inhibition (koff = 5x10-3s-1), wikiwiki (kon = 1.7x107 mol/L-1 s-1), a ma ke ʻano hilinaʻi ʻana (Ki = 0.4 nmol/L).Ke aʻo ʻia nei ʻo Rivaroxaban no ka mālama ʻana i ka VTE, ka pale ʻana i nā hanana cardiovascular i nā maʻi me ka maʻi maʻi coronary acute, ka pale ʻana i ka hahau ʻana i nā maʻi me ka fibrillation atrial.

Kuhikuhi

ʻO Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, a me Volker Laux.ʻO Rivaroxaban: kahi mea paʻa oral factor Xa inhibitor.Arterioscler Thromb Vasc Biol 2010;30(3): 376-381

wehewehe

ʻO Rivaroxaban (BAY 59-7939) kahi mea ikaika loa，koho a pololei Factor Xa (FXa) inhibitor, e hoʻokō i ka waiwai ikaika i ka anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

In Vitro

ʻO Rivaroxaban (BAY 59-7939) he waha, pololei Factor Xa (FXa) inhibitor i ka hoʻomohala ʻana no ka pale ʻana a me ka mālama ʻana i ka thrombosis arterial a me venous.Rivaroxaban competitively inhibits kanaka FXa (Ki 0.4 nM) me> 10 000-fold oi koho ma mua o ka serine proteases;ke pale aku nei i ka hana prothrombinase (IC50 2.1 nM).Rivaroxaban inhibits endogenous FXa oi potently i loko o ke kanaka a me ka rabbit plasma (IC50 21 nM) ma mua o rat plasma (IC50 290 nM).Hōʻike ia i nā hopena anticoagulant i loko o ka plasma kanaka, pālua ka manawa prothrombin (PT) a hoʻāla i ka manawa thromboplastin hapa ma 0.23 a me 0.69.μM, kēlā me kēia.

ʻO Rivaroxaban (BAY 59-7939) he mea ikaika a koho, kuhikuhi FXa inhibitor me ka maikaʻi o ka hana vivo a me ka bioavailability oral maikaʻi.Rivaroxaban (BAY 59-7939), lawelawe ʻia e iv bolus ma mua o ka thrombus induction, hoʻemi i ka thrombus form (ED50 0.1 mg / kg), inhibits FXa, a hoʻolōʻihi i ka dosis PT ma muli o ka hilinaʻi.Hoʻopilikia iki ʻia ʻo PT a me FXa i ka ED50 (1.8-fold piʻi a me 32% inhibition, kēlā me kēia).Ma ka 0.3 mg / kg (ke kumu e alakaʻi ai i ka hoʻopau piha ʻana i ka hoʻokumu ʻana o ka thrombus), hoʻolōʻihi ʻia ʻo Rivaroxaban i ka PT (3.2).±0.5-fold) a pale i ka hana FXa (65±3%).

Waihona

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