Apixaban CAS: 503612-47-3
MF: C25H25N5O4
MW: 459.50
A highly selective, reversible, and direct inhibitor of Factor X.

Apixaban (CAS 503612-47-3)

Apixaban | CAS 503612-47-3 is rated 5.0 out of 5 by 1.
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Synonym: BMS-562247
Application: A highly selective, reversible, and direct inhibitor of Factor X
CAS Number: 503612-47-3
Purity: ≥98%
Molecular Weight: 459.50
Molecular Formula: C25H25N5O4
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

Apixaban is a highly selective, reversible, and direct inhibitor of Human Factor X and Rabbit Factor X with Ki of 0.08 nM and 0.17 nM, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor X with Ki of 0.08 nM and 0.17 nM for Human Factor X and Rabbit Factor X, respectively. In vitro, Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays.


References

PMID: 17914785 PMID: 18315548 PMID: 19851712 PMID: 21461793

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (18 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), DMF (~3 mg/ml), and 1:1 solution of DMSO: PBS (pH 7.2) (~0.5 mg/ml).
Storage :
Store at 4° C
Melting Point :
326.53° C (Predicted)
Boiling Point :
~770.5° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
IC50 :
European rabbit: EC5050 = 325 nM; Thrombus formation in rabbit arteriovenous shunt thrombosis model: IC50 = 329 nM (European rabbit)
Ki Data :
Factor Xa: Ki= 0.08 nM (human); Factor Xa: Ki= 0.17 nM (rabbit); Thrombin: Ki= 3.1 µM (human)
pK Values :
pKb: 0.81 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
10182969
MDL Number :
MFCD11977295
SMILES :
COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N

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Certificate of Analysis

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Apixaban  Product Citations

See how others have used Apixaban. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 25294586  Ishibashi, Y. et al. 2014. Thrombosis research. 134: 1365-7.

PMID: # 31816472  J Pharm Biomed Anal. 179: 112992.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Wong et al Wong et al. (PubMed ID 18315548) found that Apixaban prevented thrombosis in rabbits via FXa inhibition. -SCBT Publication Review
Date published: 2015-07-15
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