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i-dabigatran etexilate (CAS# 211915-06-9)

Isakhiwo Samakhemikhali:

I-Molecular Formula I-C34H41N7O5
I-Molar Mass 627.73
Ukuminyana 1.24±0.1 g/cm3(Kubikezelwe)
I-Melting Point 128-129°
I-Boling Point 827.9°C ku-760 mmHg
I-Flash Point 454.5°C
Ukuncibilika I-DMSO (Kancane), i-Methanol (Kancane)
I-Vapor Presure 1.49E-27mmHg ku-25°C
Ukubukeka Okuqinile
Umbala Okumhlophe kuya Kuphuzi Okuphaphathekile
pKa 9.88±0.46(Okubikezelwe)
Isimo Sesitoreji Ivalwe endaweni eyomile, Gcina efrijini, ngaphansi kuka -20°C
Ukuzinza I-Hygroscopic
I-Refractive Index 1.614
Isifundo se-in vitro I-Dabigatran ikhetha ngokukhetha nangokuhlehlisa i-thrombin yomuntu (Ki: 4.5 nM) kanye nokuhlanganiswa kweplatelet eyenziwe yi-thrombin (IC50: 10 nM) futhi ayinawo umthelela ovimbelayo kwamanye ama-ejenti avuselela i-platelet. I-Dabigatran ivimbela ukukhiqizwa kwe-(PPP) i-thrombin ku-plasma yamaplatelet aphelile nge-IC50 ye-0.56 μm njengoba kukalwa nge-endogenous thrombin Index (ETP). Ukuhlolwa kwe-in vitro, i-Dabigatran inomphumela we-anticoagulant oncike ekugxilweni ezinhlobonhlobo ezihlukahlukene. Ku-PPP yomuntu, isikhathi se-thromboplastin esiyingxenye esicushiwe (aPTT), isikhathi se-prothrombin (PT) siphindwe kabili ekugxilweni kuka-0.23,0.83 no-0.18 μm, ngokulandelana. Futhi i-Ecarin clotting time (ECT)..
Isifundo se-vivo I-Dabigatran incike kumthamo ende we-APPT ngemuva kokuphathwa komthambo wamagundane (0.3,1 kanye no-3 mg/kg) nezinkawu ze-rhesus (0.15,0.3 kanye no-0.6 mg/kg). I-Dabigatran etexilate (20 mg/kg, PO) ikhiqize ukwanda okuncane kwenani lika-k kanye nokuncishiswa okuncane kokwanda okukhulu kwezingulube kune-enoxaparin. I-Dabigatran(0.01-0.1 mg/kg) i-thrombosis encishisiwe encishisiwe umthamo, ne-ED50 (umthamo osebenzayo wama-50%) ube ngu-0.033 mg/kg kanye nokuvinjelwa okuphelele ku-0.1 mg/kg. I-Dabigatran etexilate (5-30 mg/kg) ivimbele ukwakheka kwe-thrombus ngendlela encike kumthamo kanye nesikhathi, ngokuvinjelwa okukhulu okwenzeka ngemva kwemizuzu engama-30 yokwelashwa kwangaphambili, okubonisa umphumela wokusebenza ngokushesha.

Imininingwane Yomkhiqizo

Omaka bomkhiqizo

 

Isingeniso

I-Dibutyl phthalate iyinhlanganisela yezinto eziphilayo. Iwuketshezi oluphuzi olukhanyayo olungenambala olunephunga elikhethekile.

 

I-Dabigatran etexilate isetshenziswa kakhulu njenge-plasticizer. Ingakwazi ukuthuthukisa ukuthamba kanye ne-ductility yamapulasitiki, ngakho-ke isetshenziswa kakhulu ekwenzeni imikhiqizo yepulasitiki, njengamafilimu epulasitiki, amapayipi epulasitiki, i-plastic flooring nezicathulo zepulasitiki. Ingasetshenziswa futhi njengesengezo kwizincibilikisi, izinto zokugcoba neziqholo.

 

I-Dabigatran etexilate ngokuvamile ilungiswa ngokufakwa kwe-phthalic anhydride nge-n-butanol noma i-isobutanol. Ukusabela ngokuvamile kwenziwa phambi kwe-acid catalyst ezingeni lokushisa elifanele kanye nokucindezela.

Kungacasula isikhumba namehlo futhi kufanele kuhlanjululwe ngamanzi amaningi ngokushesha ngemva kokuthintana. Gwema ukusabela ngama-oxidants, ugweme imithombo yokuthungela futhi kude namazinga okushisa aphezulu namalangabi avulekile phakathi nokusebenza nokugcinwa. Kufanele kungene umoya kahle ngesikhathi sokusetshenziswa ukuze kugwenywe ukunqwabelana komhwamuko.

 


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