Apixaban is a highly selective, reversible Factor Xa inhibitor with Ki of 0.08 nM and 0.17 nM in humans and rabbits, respectively.

 

Brand: BCM

 

Target: Factor Xa

 

Signaling Pathways: Metabolism

 

In Vitro: Apixaban has excellent pharmacokinetic properties in dogs: very low clearance (Cl: 0.02 L/kg/h), low volume distribution (Vdss: 0.2 L/kg), half-life (T1/2: 5.8 h) and oral bioavailability (F: 58%). In rabbit models of venous thrombosis, arteriovenous shunt thrombosis and electrically mediated carotid thrombosis,Apixaban showed antithrombotic activity with EC50 of 110 nM,270 nM and 70 nM, respectively.

 

In Vivo: Apixaban prolonged human clotting time by doubling prothrombin time (3.6 μM), modified prothrombin time (0.37 μM), activated partial thromboplastin time (7.4 μM) and HepTest (0.4 μM) in normal human plasma in vitro. Apixaban was highly selective for human and rabbit Factor Xa inhibition with Ki of 0.08 and 0.17 nM, respectively. In addition, in the PT and APTT experiments,Apixaban had the highest utility for human and rabbit plasma, and was less effective for rat and dog plasma.

 

Melting Point: 235-238°C

 

Boiling Point: 770.5±60.0 °C(Predicted)

 

pKa: 15.01±0.20(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS08

 

Isomeric SMILES: COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N  

 

InChIKey: QNZCBYKSOIHPEH-UHFFFAOYSA-N  

 

InChI: InChI=1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)

 

Attribute
[Chem Name]	1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[3,4-c]pyridine-3-carboxamide
[Synonym]	Apixaban; BMS 562247-01
[CAS No.]	503612-47-3
[EINECS]	639-684-6
[MDL No.]	MFCD11977295
[Formula]	C25H25N5O4
[Molecular]	459.5
[Form]	White to Off-White Solid
[Storage]	Sealed in dry. Store in freezer, under -20°C

Goods Tag