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Apixaban

Catalog No. T1736 CAS 503612-47-3

Synonyms: BMS-562247-01

Apixaban (BMS-562247-01) is an orally active inhibitor of coagulation factor Xa with anticoagulant activity. Apixaban directly inhibits factor Xa, thereby interfering with the conversion of prothrombin to thrombin and preventing the formation of cross-linked fibrin clots.

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Apixaban, CAS 503612-47-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 45.00
10 mg	In stock	$ 54.00
50 mg	In stock	$ 72.00
500 mg	In stock	$ 98.00
1 g	In stock	$ 148.00
1 mL * 10 mM (in DMSO)	In stock	$ 55.00

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Purity: 100%

Purity: 99.7%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Apixaban (BMS-562247-01) is an orally active inhibitor of coagulation factor Xa with anticoagulant activity. Apixaban directly inhibits factor Xa, thereby interfering with the conversion of prothrombin to thrombin and preventing the formation of cross-linked fibrin clots.
Targets&IC50	FXa (rabbit):0.17 nM(Ki), FXa (human):0.08 nM(Ki)
In vitro	Apixaban demonstrates excellent pharmacokinetic properties in dogs, characterized by very low clearance (Cl: 0.02 L/kg/h), low volume of distribution (Vdss: 0.2 L/kg), a half-life (T1/2: 5.8 h), and oral bioavailability (F: 58%). Its antithrombotic efficacy is evident in models of venous thrombosis, arteriovenous shunt thrombosis, and electrically induced carotid artery thrombosis in rabbits, with EC50 values of 110 nM, 270 nM, and 70 nM, respectively.
In vivo	When applied to normal human plasma in vitro, Apixaban extends coagulation time, doubling the prothrombin time (3.6 μM), modified prothrombin time (0.37 μM), activated partial thromboplastin time (7.4 μM), and HepTest (0.4 μM). Apixaban exhibits high selectivity in inhibiting human and rabbit Factor Xa, with Ki values of 0.08 and 0.17 nM, respectively. Additionally, Apixaban demonstrates maximum effectiveness in human and rabbit plasma in PT (Prothrombin Time) and APTT (Activated Partial Thromboplastin Time) assays, with comparatively lesser effects observed in rat and dog plasma.
Kinase Assay	Purified FXa is obtained after activation with Russell's viper venom followed by affinity chromatography. The resulting FXa is > 95% pure as judged by sodium dodecylsulfate polyacrylamide gel electrophoresis. The substrate affinity values for FXa, expressed as the Michaelis-Menten-Henri constant (Km), for human, rabbit, rat and dog FXa are determined using the chromogenic substrate S-2765, and are 36, 60, 240 and 70 μM, respectively. The substrate hydrolysis is monitored by measuring absorbance at 405 nm at 25°C for up to 30 min using a SpectraMax 384 Plus plate reader and SoftMax. FXa activity for each substrate and inhibitor concentration pair is determined in duplicate. The Ki values are calculated by non-linear least-squares fitting of the steady-state substrate hydrolysis rates to the equation for competitive inhibition (Equation 1) using GRAFIT, where v equals reactions velocity in OD min?1, Vmax equals maxiumum reaction velocity, S equals substrate concentration, and I equals inhibitor concentration.

Synonyms	BMS-562247-01
Molecular Weight	459.5
Formula	C25H25N5O4
CAS No.	503612-47-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 15 mg/mL (32.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Pinto DJ, et al. J Med Chem. 2007, 50(22), 5339-5356. 2. Wong PC, et al. J Thromb Haemost. 2008, 6(5), 820-829. 3. Zhang D, et al. J Thromb Thrombolysis. 2010, 29(1), 70-80. 4. He K, et al. Eur J Drug Metab Pharmacokinet. 2011, 36(3), 129-139.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Inhibitor Library FDA-Approved Drug Library Bioactive Compound Library Coagulation and Anticoagulation Compound Library Pediatric Drug Library Human Metabolite Library Clinical Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Apixaban 503612-47-3 Metabolism Factor Xa Fxa Inhibitor rabbit clotting Factor plasma BMS-562247-01 human EC2x inhibit inhibitor

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