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ibicuruzwa

dabigatran etexilate (CAS # 211915-06-9)

Umutungo wa Shimi:

Inzira ya molekulari C34H41N7O5
Misa 627.73
Ubucucike 1.24 ± 0.1 g / cm3 (Biteganijwe)
Ingingo yo gushonga 128-129 °
Ingingo ya Boling 827.9 ° C kuri 760 mmHg
Flash point 454.5 ° C.
Gukemura DMSO (Buhoro), Methanol (Buhoro)
Umwuka 1.49E-27mmHg kuri 25 ° C.
Kugaragara Birakomeye
Ibara Umweru kugeza Umuhondo
pKa 9.88 ± 0.46 (Byahanuwe)
Imiterere y'Ububiko Ikidodo cyumye, Ubike muri firigo, munsi ya -20 ° C.
Igihagararo Hygroscopique
Ironderero 1.614
Mu bushakashatsi bwa vitro Dabigatran ihitamo kandi ihindura ibuza trombine yumuntu (Ki: 4.5 nM) hamwe na trombine iterwa na platine (IC50: 10 nM) kandi nta ngaruka zibuza izindi mikorere itera platine. Dabigatran ibuza kubyara (PPP) trombine muri plasma ya platine yatakaye hamwe na IC50 ya 0.56 μ m nkuko byapimwe na endogenous trombin Index (ETP). Mu bushakashatsi bwa vitro, Dabigatran igira ingaruka ziterwa na anticoagulant yibinyabuzima bitandukanye. Muri PPP yumuntu, igihe cyakoreshwaga igice cya tromboplastine (aPTT), igihe cya prothrombine (PT) cyikubye kabiri kuri 0.23,0.83 na 0.18 mm. Na Ecarin igihe cyo kwambara (ECT) ..
Mu bushakashatsi bwa vivo Dabigatran dose-biterwa na APPT igihe kirekire nyuma yubuyobozi bwimitsi yimbeba (0.3,1 na 3 mg / kg) hamwe ninguge za rhesus (0.15,0.3 na 0,6 mg / kg). Dabigatran etexilate (20 mg / kg, PO) yabyaye igihe kirekire cyo k agaciro no kutiyongera kwinshi kwingurube kurusha enoxaparine. Dabigatran (0.01-0.1 mg / kg) ikigereranyo cyatewe na trombose, hamwe na ED50 (50% ikoreshwa neza) ni 0.033 mg / kg kandi kubuza byuzuye kuri 0.1 mg / kg. Dabigatran etexilate (5-30 mg / kg) yabujije gukora trombus muburyo bwa dose-kandi biterwa nigihe, hamwe no kubuzwa gukabije bibaho nyuma yiminota 30 yo kwitegura, byerekana ingaruka zihuse.

Ibicuruzwa birambuye

Ibicuruzwa

 

Intangiriro

Dibutyl phthalate nikintu kama. Nibara ritagira ibara ryoroshye ryumuhondo hamwe nimpumuro idasanzwe.

 

Dabigatran etexilate ikoreshwa cyane nka plastike. Irashobora kongera ubworoherane no guhindagurika kwa plastiki, bityo ikoreshwa cyane mugukora ibicuruzwa bya pulasitike, nka firime ya plastike, imiyoboro ya pulasitike, hasi ya plastike ninkweto za plastiki. Irashobora kandi gukoreshwa nk'inyongeramusaruro, amavuta n'impumuro nziza.

 

Dabigatran etexilate mubisanzwe itegurwa na esterification ya phthalic anhydride hamwe na n-butanol cyangwa isobutanol. Ubusanzwe reaction ikorwa imbere ya catisale ya acide kubushyuhe bukwiye hamwe nigitutu.

Irashobora kurakaza uruhu n'amaso kandi igomba kwozwa namazi menshi mukimara guhura. Irinde kwitwara hamwe na okiside, wirinde inkongi y'umuriro kandi kure yubushyuhe bwinshi n'umuriro ugurumana mugihe cyo gukora no kubika. Igomba guhumeka neza mugihe cyo gukoresha kugirango wirinde guhumeka.

 


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