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dabigatran etexilate (CAS# 211915-06-9) Umfanekiso okhoyo
  • dabigatran etexilate (CAS# 211915-06-9) 1

dabigatran etexilate (CAS# 211915-06-9)

Ipropati yeMichiza:

Ifomula yeemolekyuli C34H41N7O5
IMisa yeMolar 627.73
Ukuxinana 1.24±0.1 g/cm3(Kuxelwe kwangaphambili)
Indawo yokunyibilika 128-129 °
Indawo yeBoling 827.9 ° C kwi-760 mmHg
Indawo yokuflasha 454.5°C
Ukunyibilika I-DMSO (Kancinci), iMethanol (Kancinci)
Uxinzelelo loMphunga 1.49E-27mmHg ku-25°C
Imbonakalo Iqinile
Umbala Mhlophe ukuya koMthubi
pKa 9.88±0.46(Kuxelwe kwangaphambili)
Imeko yoGcino Itywinwe kwindawo eyomileyo, Gcina kwisikhenkcisi, ngaphantsi kwe -20°C
Uzinzo Hygroscopic
Refractive Index 1.614
Isifundo se-in vitro I-Dabigatran ikhetha kwaye ibuyisela umva inqanda i-thrombin yomntu (i-Ki: 4.5 nM) kunye ne-thrombin-induced platelet aggregation (IC50: 10 nM) kwaye ayinayo impembelelo yokuthintela kwezinye iiplatelet stimulating agents. I-Dabigatran inqanda ukuveliswa kwe-thrombin (PPP) kwi-plasma yeeplatelet eziphelile kunye ne-IC50 ye-0.56 μm njengoko ilinganiswe yi-Endogenous thrombin Index (ETP). Uvavanyo lwe-in vitro, i-Dabigatran inefuthe elixhomekeke kwi-anticoagulant kwiintlobo ezahlukeneyo. Kwi-PPP yomntu, ixesha elisebenzayo le-thromboplastin (aPTT), ixesha le-prothrombin (PT) liphindwe kabini kwi-concentrations ye-0.23,0.83 kunye ne-0.18 μm, ngokulandelanayo. Kwaye ixesha lokujika kwe-Ecarin (ECT) ..
Kwisifundo se-vivo I-Dabigatran dose-ixhomekeke kwi-APPT yexesha elide emva kokulawulwa kwe-intravenous kwiigundane (0.3,1 kunye ne-3 mg / kg) kunye ne-rhesus monkeys (0.15,0.3 kunye ne-0.6 mg / kg). I-Dabigatran etexilate (i-20 mg / kg, i-PO) ivelise ukwanda okuncinci kwexabiso le-k kunye nokunciphisa okuncinci kokunyuka okuphezulu kweehagu kune-enoxaparin. I-Dabigatran (0.01-0.1 mg / kg) i-dose-dependent-dependent thrombosis, kunye ne-ED50 (i-50% i-dose esebenzayo) ibe yi-0.033 mg / kg kunye nokuvinjelwa okupheleleyo kwi-0.1 mg / kg. I-Dabigatran etexilate (i-5-30 mg / kg) inqanda ukubunjwa kwe-thrombus kwi-dose-kunye nokuxhomekeka kwexesha, kunye ne-inhibition enkulu eyenzekayo emva kwe-30 min ye-pretreatment, ebonisa umphumo osebenza ngokukhawuleza.

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Intshayelelo

I-Dibutyl phthalate yi-organic compound. Lulwelo olungenambala ukuya kumthubi olukhanyayo kunye nevumba elikhethekileyo.

 

I-Dabigatran etexilate isetyenziswa kakhulu njengeplastiki. Inokuphucula ukuthamba kunye ne-ductility yeeplastiki, ngoko isetyenziswa ngokubanzi ekwenzeni iimveliso zeplastiki, ezifana neefilimu zeplastiki, imibhobho yeplastiki, umgangatho weplastiki kunye nezihlangu zeplastiki. Isenokusetyenziswa njengesongezelelo kwizinyibilikisi, izithambisi kunye neziqholo.

 

I-Dabigatran etexilate idla ngokulungiswa nge-esterification ye-phthalic anhydride nge-n-butanol okanye i-isobutanol. Ukusabela ngokuqhelekileyo kuqhutyelwa phambi kwe-acid catalyst kwiqondo lokushisa elifanelekileyo kunye noxinzelelo.

Inokucaphukisa ulusu kunye namehlo kwaye kufuneka ihlanjululwe ngamanzi amaninzi ngokukhawuleza emva kokudibanisa. Kuphephe ukusabela nge-oxidants, ukuphepha imithombo yokutshisa kwaye kude namaqondo obushushu aphezulu kunye namadangatye avulekileyo ngexesha lokusebenza kunye nokugcinwa. Kufuneka kungene umoya kakuhle ngexesha lokusetyenziswa ukuthintela ukuqokeleleka komphunga.

 

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