Rivaroxaban

Whakaahuatanga Poto:

Ingoa o API Tohu Whakatakotoranga US DMF  EU DMF  CEP
Rivaroxaban Anticoagulant I-Roto TDP    

Taipitopito Hua

Tohu Hua

WHAKAWEHE KOREUTU

Papamuri

Rivaroxaban, 5-chloro-N - [[(5S) -2-oxo-3- [4- (3-oxomorpholin-4-yl) phenyl] -1,3-oxazolidin-5-yl] methyl] thiophene-2 -carboxamide, he kaha-aukati iti-aukati i te tauwehenga Xa he take whakakao i te waa tino nui i te ara whakaheke toto e hua ana te whakatipuranga o te thrombin me te hanganga o te poka. Ka herea a Rivaroxaban ki te Tyr288 kei roto i te pute S1 o te tauwehenga Xa na roto i te taunekeneke a Tyr288 me te putunga o te haumanu o te ngakau o te chlorothiophene. Ko te aukati ka taea te whakahoki (koff = 5x10-3s-1), tere (kon = 1.7x107 mol / L-1 s-1), a, me te tikanga whakawhirinaki (Ki = 0.4 nmol / L). I tenei wa kei te maatauhia a Rivaroxaban mo te whakaora i te VTE, te aukati i nga mahi a Cardiary ki nga tuuroro e pa ana ki te mate tuuturu, me te aukati i te whiu o nga tuuroro me te whakapakaritanga o te whenua.

Tohutoro

Ko Erihapeti Perzborn, ko Susanne Roehrig, ko Alexander Straub, ko Dagmar Kubitza, ko Wolfgang Mueck, ko Volker Laux. Rivaroxaban: he aukati Xa take a-waha hou. Arterioscler Thromb Vasc Biol 2010; 30 (3): 376-381

Whakaahuatanga

Ko Rivaroxaban (BAY 59-7939) he tino kaha,he kaitautoko me te tika Factor Xa (FXa) aukati, kia kaha te whiwhi i te kaha anti-FXa (IC50 0.7 nM; Ki 0.4 nM).

 

I Vitro

Ko te Rivaroxaban (BAY 59-7939) he aukati, ko te Tohu Xa (FXa) te aukati i te whanaketanga mo te aukati me te whakamaimoa i te thrombosis arterial me te venous trombosis. Ka aukati a Rivaroxaban i te FXa tangata (Ki 0.4 nM) me te> 10 000-whaainga nui ke atu i etahi atu proteine ​​serine; ka aukati hoki i te mahinga prothrombinase (IC50 2.1 nM). Ko te Rivaroxaban e aukati ana i te FXa endogenous kia kaha ake i roto i te plasma tangata me te koni (IC50 21 nM) i te plasma kiore (IC50 290 nM). Ka whakaatuhia nga paanga anticoagulant i te plasma tangata, te rearua i te waa prothrombin (PT) ka whakahohe i te wa thromboplastin wahanga i te 0.23 me te 0.69μM, takitahi.

 

Ko te Rivaroxaban (BAY 59-7939) he kaha, he kowhiri hoki, he kaitautoko FXa tika me te tino mahi hihiko me te koiora koiora-a-waha. Ko te Rivaroxaban (BAY 59-7939), e whakahaerehia ana e iv bolus i mua i te whakauru mai o te thrombus, ka whakaitihia te hanga trombus (ED50 0.1 mg / kg), ka aukati i te FXa, ka whakaroa i te horopeta PT. PT me FXa e raru ana i te ED50 (1.8-piki whakarakei me te 32% aukati, ia) I te 0.3 mg / kg (te horopeta e tata ana ki te aukati i te hanga trombus), ka whakaroa e Rivaroxaban te PT (3.2±0.5-hepe) ka aukati i te mahi FXa (65±3%).

 

Rokiroki

Paura

-20 ° C

3 tau
 

4 ° C

2 tau
I roto i te whakarewa

-80 ° C

6 marama
 

-20 ° C

1 marama

Hanganga matū

Rivaroxaban

WHAKAMAHI

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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