Dabigatran

Bezeichnung:Dabigatran

CAS-Nr211914-51-1

Englisch Name:Dabigatran

CBNumberCB61458206

SummenformelC25H25N7O3

Molgewicht471.51

MOL-Datei211914-51-1.mol

Dabigatran physikalisch-chemischer Eigenschaften

Schmelzpunkt	268-272°C
Siedepunkt	797.1±70.0 °C(Predicted)
Dichte	1.38±0.1 g/cm3(Predicted)
storage temp.	Keep in dark place,Inert atmosphere,Room temperature
Löslichkeit	Aqueous Acid
Aggregatzustand	Solid
pka	4.17±0.10(Predicted)
Farbe	White to Brown

Sicherheit

Giftige Stoffe Daten

211914-51-1(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Dabigatran Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
Tan Solid
Verwenden
Nonpeptide, direct thrombin inhibitor. Antithrombotic.
Verwenden
BIBR 953 (Dabigatran, Pradaxa) is potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM
Definition
ChEBI: An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-b ta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism.
Biologische Aktivität
bibr 953 is a potent, reversible, and direct inhibitor of thrombin with ic50 value of 9.3nm [1].bibr 953 shows a favorable selectivity profile and strong activity in vitro with a ki value of 4.5nm. it also exhibits the best activity profile in vivo following administration to rats. bibr 953 is designed to be converted into an orally active prodrug bibr 1048 due to its highly polar, zwitterionic nature and poor oral absorption. bibr 953 inhibits thrombin in a competitive fashion. this inhibition is rapid and reversible. bibr 953 inhibits both clot-bound and free thrombin. bibr 953 is demonstrated to have an anticoagulant efficacy both in vitro and ex vivo. since thrombin can affect cell behavior and response in various tissue types via par signaling, bibr 953 is found to be beneficial in many diseases including inflammation, infection, fibrosis and cancer.
target
thrombin
Einzelnachweise
[1] hauel nh, nar h, priepke h, ries u, stassen jm, wienen w. structure-based design of novel potent nonpeptide thrombin inhibitors. j med chem. 2002 apr 25;45(9):1757-66.
[2] van ryn j, goss a, hauel n, wienen w, priepke h, nar h, clemens a. the discovery of dabigatran etexilate. front pharmacol. 2013 feb 12;4:12.

Dabigatran Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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