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dabigatran etexilate (CAS# 211915-06-9)

Hantida Kiimikada:

Qaanuunka molecular C34H41N7O5
Molar Mass 627.73
Cufnaanta 1.24±0.1 g/cm3 (La saadaaliyay)
Meesha dhalaalaysa 128-129°
Boling Point 827.9°C at 760mmHg
Barta Fiishka 454.5°C
Solubility DMSO (wax yar), Methanol (wax yar)
Uumiga Uumiga 1.49E-27mmHg at 25°C
Muuqashada Adag
Midabka Cadaan ilaa Jaalle cirro leh
pKa 9.88±0.46 (La saadaaliyay)
Xaalada Kaydinta Waxaa lagu xidhay qalalan, ku kaydi qaboojiyaha, ka hooseeya -20 ° C
Xasilooni Hygroscopic
Tusmada Dib-u-celinta 1.614
Barashada in vitro Dabigatran si door ah oo dib-u-celin ah waxay u joojisaa thrombin bini'aadamka (Ki: 4.5 nM) iyo isku-darka trombobin-induced platelet (IC50: 10 nM) mana laha wax saameyn ah oo xannibaya wakiilada kale ee kicinta platelet. Dabigatran waxay joojisaa jiilka (PPP) trombobin ee balasmaha ee platelet-ka yaraaday ee leh IC50 ee 0.56 μm sida lagu qiyaaso index thrombin endogenous (ETP). Tijaabooyin gudaha vitro ah, Dabigatran waxay leedahay saameyn ku-tiirsanaanta xinjirowga lidka ku ah ee noocyada kala duwan. PPP-ga bini'aadamka, wakhtiga qayb ka mid ah thromboplastin ee firfircoon (aPTT), wakhtiga prothrombin (PT) ayaa la labanlaabay xajmiyada 0.23,0.83 iyo 0.18 μm, siday u kala horreeyaan. Iyo Ecarin xinjirowga waqtiga (ECT).
In vivo waxbarasho Dabigatran dose-ku-tiirsanaanta ku-tiirsanaanta dheer ee PPT ka dib maamulka xididka ee jiirka (0.3,1 iyo 3 mg/kg) iyo daanyeerka rhesus (0.15,0.3 iyo 0.6 mg/kg). Dabigatran etexilate (20 mg / kg, PO) waxay soo saartey kordhin yar oo k qiimaha k iyo hoos u dhigista korodhka ugu badan ee doofaarka marka loo eego enoxaparin. Dabigatran (0.01-0.1 mg / kg) qiyaasta ku-tiirsanaanta hoos u dhaca xinjirowga dhiigga, oo leh ED50 (50% qiyaasta waxtarka leh) oo ah 0.033 mg / kg iyo xannibaad dhammaystiran oo ah 0.1 mg / kg. Dabigatran etexilate (5-30 mg / kg) waxay joojisay samaynta xinjirowga dhiigga ee qiyaasta-iyo wakhti ku-tiirsanaanta, iyada oo la xakameynayo ugu badnaan ka dib 30 min ee ka-hortagga, taas oo muujinaysa saameyn degdeg ah.

Faahfaahinta Alaabta

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Hordhac

Dibutyl phthalate waa iskudhis organic ah. Waa dareere huruud ah oo aan midab lahayn oo iftiin leh oo leh udgoon gaar ah.

 

Dabigatran etexilate waxaa inta badan loo isticmaalaa sidii balaastiiste ahaan. Waxay kor u qaadi kartaa jilicsanaanta iyo ductility balaastikada, sidaas darteed waxaa si ballaaran loo isticmaalaa soo saarista alaabta caaga ah, sida filimada caagga ah, tuubooyinka caagga ah, sagxadaha caagga ah iyo kabaha caagga ah. Waxa kale oo loo isticmaali karaa wax lagu daro dareerayaasha, saliidaha iyo udgoonka.

 

Dabigatran etexilate waxaa sida caadiga ah lagu diyaariyaa esterification of phthalic anhydride leh n-butanol ama isobutanol. Dareen-celinta waxaa sida caadiga ah lagu fuliyaa joogitaanka kicinta aashitada heerkulka ku habboon iyo cadaadiska.

Waxay noqon kartaa mid ka xanaajisa maqaarka iyo indhaha waana in lagu luqluqiyaa biyo badan isla markaaba marka la taabto. Ka fogow in aad la falgasho oksaydhiyeyaasha, ka fogaanshaha ilaha dabka kana fogow heerkulka sare iyo ololka furan inta lagu jiro hawlgalka iyo kaydinta. Waa in si fiican loo neefsadaa marka la isticmaalayo si looga fogaado ururinta uumiga.

 


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