Tuam Tshoj Rivaroxaban tuam ntxhab thiab cov muag khoom

Rivaroxaban

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API lub npe	Qhov taw qhia	Specification	US DMF	EU DMF	CEP
Rivaroxaban	Anticoagulant	Hauv tsev	TDP

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Product Detail

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Keeb kwm

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, yog ib qho muaj zog me me-molecule inhibitor ntawm yam Xa uas yog qhov ua rau coagulation ntawm qhov tseem ceeb hauv cov ntshav coagulation txoj hauv kev uas ua rau muaj kev tsim cov ntshav coagulation. thrombin thiab tsim cov hlab ntsha. Rivaroxaban khi rau Tyr288 hauv S1 hnab tshos ntawm yam Xa los ntawm kev sib cuam tshuam ntawm Tyr288 thiab cov tshuaj chlorine hloov ntawm chlorothiophene moiety. Qhov inhibition yog thim rov qab (koff = 5x10-3s-1), ceev (kon = 1.7x107 mol / L-1 s-1), thiab nyob rau hauv ib qho concentration-dependent yam (Ki = 0.4 nmol / L). Rivaroxaban tam sim no tab tom kawm txog kev kho mob ntawm VTE, kev tiv thaiv kab mob plawv hauv cov neeg mob uas mob hlab ntsha tawg, tiv thaiv mob stroke hauv cov neeg mob atrial fibrillation.

Kev siv

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, thiab Volker Laux. Rivaroxaban: qhov ncauj tshiab Xa inhibitor. Arterioscler Thromb Vasc Biol 2010; 30(3): 376-381

Kev piav qhia

Rivaroxaban (BAY 59-7939) yog ib qho muaj zog heev,xaiv thiab ncaj qha Factor Xa (FXa) inhibitor, ua tiav qhov muaj zog hauv kev tiv thaiv FXa potency (IC50 0.7 nM; Ki 0.4 nM).

Hauv Vitro

Rivaroxaban (BAY 59-7939) yog qhov ncauj, ncaj qha Factor Xa (FXa) inhibitor hauv kev txhim kho rau kev tiv thaiv thiab kho cov hlab ntsha thiab venous thrombosis. Rivaroxaban sib tw inhibits tib neeg FXa (Ki 0.4 nM) nrog> 10 000-fold ntau dua selectivity dua rau lwm cov serine proteases; Nws kuj inhibits kev ua haujlwm prothrombinase (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa ntau zog nyob rau hauv tib neeg thiab luav plasma (IC50 21 nM) dua nas plasma (IC50 290 nM). Nws qhia txog cov teebmeem anticoagulant hauv tib neeg plasma, ob npaug ntawm lub sijhawm prothrombin (PT) thiab ua kom lub sijhawm thromboplastin ib nrab ntawm 0.23 thiab 0.69.μM, raws.

Rivaroxaban (BAY 59-7939) yog lub zog thiab xaiv, ncaj qha FXa inhibitor nrog zoo heev hauv vivo kev ua si thiab qhov ncauj zoo bioavailability. Rivaroxaban (BAY 59-7939), tswj los ntawm iv bolus ua ntej thrombus induction, txo thrombus tsim (ED50 0.1 mg / kg), inhibits FXa, thiab prolongs PT koob tshuaj nyob ntawm seb. PT thiab FXa cuam tshuam me ntsis ntawm ED50 (1.8-fold nce thiab 32% inhibition, feem). Ntawm 0.3 mg / kg ( koob tshuaj ua rau yuav luag tag nrho inhibition ntawm thrombus tsim), Rivaroxaban me ntsis prolongs PT (3.2).±0.5-fold) thiab inhibits FXa kev ua haujlwm (65±3%).

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