Betrixaban

Bezeichnung:Betrixaban

CAS-Nr330942-05-7

Englisch Name:Betrixaban

CBNumberCB02500171

SummenformelC23H22ClN5O3

Molgewicht451.91

MOL-Datei330942-05-7.mol

Betrixaban physikalisch-chemischer Eigenschaften

Schmelzpunkt	210-213°C
Dichte	1.30±0.1 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	11.00±0.70(Predicted)
Farbe	Off-White
CAS Datenbank	330942-05-7

Gefahreninformationscode (GHS)

Betrixaban Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Betrixaban is a novel anticoagulant, an oral direct inhibitor of factor Xa (FXa) for use in the prevention of venous thromboembolism (VTE).
Definition
ChEBI: Betrixaban is a secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade. It has a role as an anticoagulant and an EC 3.4.21.6 (coagulation factor Xa) inhibitor. It is a member of guanidines, a member of benzamides, a secondary carboxamide, a monochloropyridine and a monomethoxybenzene.
Biologische Aktivität
betrixaban is a highly potent, selective, and orally efficacious inhibitor of factor xa with ic50 value of 1.5nm [1].betrixaban shows excellent anticoagulant potency in vitro. in the rabbit deep vein thrombosis model, the concentration of betrixaban required to double the rabbit prothrombin time is below 2μm. betrixaban is selective for fxa and has poor activity for thrombin, trypsin, t-pa and apc. the patch clamp herg assay shows that betrixaban has low affinity with herg suggesting it is safer than other candidate compounds. in addition, betrixaban displays a profile of good oral bioavailability and oral exposure, long half-life in animal models. it has bioavailability of 51.6% at dose of 0.5 mg/kg iv and 2.5 mg/kg po. furthermore, the phase ii study has proved betrixaban as an oral fxa inhibitor for prevention of venous thromboembolic events [1].
Einzelnachweise
[1] zhang p, huang w, wang l, bao l, jia zj, bauer sm, goldman ea, probst gd, song y, su t, fan j, wu y, li w, woolfrey j, sinha u, wong pw, edwards st, arfsten ae, clizbe la, kanter j, pandey a, park g, hutchaleelaha a, lambing jl, hollenbach sj, scarborough rm, zhu by. discovery of betrixaban (prt054021), n-(5-chloropyridin-2-yl)-2-(4-(n,n-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor xa inhibitor. bioorg med chem lett. 2009 apr 15;19(8):2179-85.

Betrixaban Upstream-Materialien And Downstream Produkte

Betrixaban Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

330942-05-7, Betrixaban Verwandte Suche:

Send Inquriy