dabigatran etexilate (CAS# 211915-06-9)

Thepa ea Lik'hemik'hale:

Foromo ea limolek'hule	C34H41N7O5
'Misa oa Molar	627.73
Botenya	1.24±0.1 g/cm3(E boletsoeng esale pele)
Melting Point	128-129 °
Boling Point	827.9°C ho 760 mmHg
Flash point	454.5°C
Solubility	DMSO (Hanyane), Methanol (Hanyenyane)
Khatello ea Mouoane	1.49E-27mmHg ho 25°C
Ponahalo	Tiileng
Mmala	Bosoeu ho isa Bosehla bo Pehla
pKa	9.88±0.46(E boletsoeng esale pele)
Boemo ba polokelo	E tiisitsoe ka sehatsetsing, ka tlas'a -20°C
Botsitso	Hygroscopic
Refractive Index	1.614
Thuto ea in vitro	Dabigatran e thibela thrombin ea motho (Ki: 4.5 nM) ka mokhoa o khethang le ka mokhoa o feto-fetohang le thrombin-induced platelet aggregation (IC50: 10 nM) 'me ha e na phello e thibelang lintho tse ling tse susumetsang platelet. Dabigatran e thibela tlhahiso ea (PPP) thrombin ka plasma ea liplatelete tse senyehileng tse nang le IC50 ea 0.56 μm joalokaha e lekantsoe ke endogenous thrombin Index (ETP). Liteko tsa in vitro, Dabigatran e na le phello ea anticoagulant e itšetlehileng ka mefuta e fapaneng. Ho PPP ea motho, nako e kentsoeng ea karolo ea thromboplastin (aPTT), nako ea prothrombin (PT) e imetsoe habeli ka likhakanyo tsa 0.23,0.83 le 0.18 μm, ka ho latellana. Le nako ea ho koala ha Ecarin (ECT).
Thuto ea in vivo	Dabigatran e itšetlehileng ka tekanyo ea nako e telele ea APPT ka mor'a tsamaiso ea methapo ho likhoto (0.3,1 le 3 mg / kg) le litšoene tsa rhesus (0.15,0.3 le 0.6 mg / kg). Dabigatran etexilate (20 mg/kg, PO) e hlahisitse katoloso e nyane ea boleng ba k le ho fokotseha ho fokolang ha keketseho e kholo ea likolobe ho feta enoxaparin. Dabigatran (0.01-0.1 mg / kg) e itšetlehileng ka tekanyo ea thrombosis, e nang le ED50 (50% tekanyo e sebetsang) e le 0.033 mg / kg le ho thibela ka ho feletseng ho 0.1 mg / kg. Dabigatran etexilate (5-30 mg / kg) e thibela ho thehoa ha thrombus ka mokhoa o itšetlehileng ka tekanyo le nako, ka thibelo e kholo e hlahang ka mor'a metsotso e 30 ea phekolo ea pele, e bontšang phello e potlakileng ea ho sebetsa.

Re romelle lengolo-tsoibila

Lintlha tsa Sehlahisoa

Li-tag tsa Sehlahisoa

Selelekela

Dibutyl phthalate ke motsoako oa lintho tse phelang. Ke mokelikeli o mosehla o se nang 'mala o khanyang o nang le monko o khethehileng.

Dabigatran etexilate e sebelisoa haholo-holo joalo ka polasetiki. E ka ntlafatsa bonolo le ductility ea polasetiki, kahoo e sebelisoa haholo ha ho etsoa lihlahisoa tsa polasetiki, tse kang lifilimi tsa polasetiki, liphaephe tsa polasetiki, fatše le lieta tsa polasetiki. E ka boela ea sebelisoa e le motsoako oa li-solvents, lubricant le monko o monate.

Dabigatran etexilate hangata e lokisoa ke esterification ea phthalic anhydride e nang le n-butanol kapa isobutanol. Hangata karabelo e etsoa ka pel'a motsoako oa asiti ka mocheso o loketseng le khatello.

E ka halefisa letlalo le mahlo 'me e lokela ho hlatsoa ka metsi a mangata hang ka mor'a ho kopana. Qoba ho sebetsana le li-oxidants, ho qoba mehloli ea ho khantša le hole le mocheso o phahameng le malakabe a bulehileng nakong ea ts'ebetso le polokelo. E lokela ho kenngoa moea o motle nakong ea tšebeliso ho qoba ho bokellana ha mouoane.

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