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dabigatran etexilate (CAS# 211915-06-9)

Chemical Property:

Molecular Formula C34H41N7O5
Molar Misa 627.73
Kuchulukana 1.24±0.1 g/cm3(Zonenedweratu)
Melting Point 128-129 °
Boling Point 827.9 ° C pa 760 mmHg
Pophulikira 454.5°C
Kusungunuka DMSO (Pang'ono), Methanol (Pang'ono)
Kuthamanga kwa Vapor 1.49E-27mmHg pa 25°C
Maonekedwe Zolimba
Mtundu White mpaka Pale Yellow
pKa 9.88±0.46 (Zonenedweratu)
Mkhalidwe Wosungira Osindikizidwa muumirira, Sungani mufiriji, pansi pa -20°C
Kukhazikika Hygroscopic
Refractive Index 1.614
Maphunziro a in vitro Dabigatran mosankha komanso mosinthika amalepheretsa thrombin yamunthu (Ki: 4.5 nM) ndi kuphatikizika kwa mapulateleti opangidwa ndi thrombin (IC50: 10 nM) ndipo ilibe cholepheretsa pazinthu zina zoyambitsa mapulateleti. Dabigatran imalepheretsa kupanga kwa (PPP) thrombin mu plasma ya mapulateleti otha omwe ali ndi IC50 ya 0.56 μm monga momwe amayezera ndi endogenous thrombin Index (ETP). Kuyesa kwa in vitro, Dabigatran imakhala ndi anticoagulant yodalira mitundu yosiyanasiyana. Mu PPP yaumunthu, nthawi yokhazikitsidwa ya thromboplastin (aPTT), nthawi ya prothrombin (PT) idachulukitsidwa pa 0.23,0.83 ndi 0.18 μm, motsatana. Ndipo Ecarin clotting nthawi (ECT).
Kuphunzira mu vivo Mlingo wa Dabigatran umadalira nthawi yayitali APPT pambuyo polowetsedwa m'mitsempha mu makoswe (0.3,1 ndi 3 mg/kg) ndi anyani a rhesus (0.15,0.3 ndi 0.6 mg/kg). Dabigatran etexilate (20 mg/kg, PO) idatulutsa kuchepa pang'ono kwa mtengo wa k komanso kuchepa pang'ono pakuwonjezeka kwakukulu kwa nkhumba kuposa enoxaparin. Dabigatran (0.01-0.1 mg/kg) mlingo umadalira kuchepa kwa thrombosis, ndi ED50 (50% mlingo wogwira) kukhala 0.033 mg/kg ndi kuletsa kwathunthu pa 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) imalepheretsa mapangidwe a thrombus mumkhalidwe wotengera nthawi komanso nthawi, ndikuletsa kwakukulu komwe kumachitika pambuyo pa mphindi 30 za pretreatment, zomwe zikuwonetsa kuchitapo kanthu mwachangu.

Tsatanetsatane wa Zamalonda

Zolemba Zamalonda

 

Mawu Oyamba

Dibutyl phthalate ndi organic pawiri. Ndi madzi achikasu owala opanda mtundu ndi fungo lapadera.

 

Dabigatran etexilate imagwiritsidwa ntchito makamaka ngati pulasitiki. Ikhoza kumapangitsanso kufewa ndi kusinthasintha kwa mapulasitiki, kotero amagwiritsidwa ntchito kwambiri popanga zinthu zapulasitiki, monga mafilimu apulasitiki, mapaipi apulasitiki, pulasitiki pansi ndi nsapato zapulasitiki. Itha kugwiritsidwanso ntchito ngati chowonjezera ku zosungunulira, mafuta onunkhira ndi zonunkhira.

 

Dabigatran etexilate nthawi zambiri imakonzedwa ndi esterification ya phthalic anhydride ndi n-butanol kapena isobutanol. Zomwe zimachitika nthawi zambiri zimachitika pamaso pa chothandizira cha asidi pa kutentha koyenera komanso kuthamanga.

Ikhoza kukwiyitsa khungu ndi maso ndipo iyenera kutsukidwa ndi madzi ambiri mutangokhudzana. Pewani kuchitapo kanthu ndi ma okosijeni, kupewa magwero oyatsira komanso kutali ndi kutentha kwambiri komanso malawi otseguka mukamagwira ntchito ndikusunga. Iyenera kukhala ndi mpweya wokwanira panthawi yogwiritsira ntchito kuti mpweya usachulukane.

 


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