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Letaxaban

Chemical Structure : Letaxaban

CAS No.: 870262-90-1

Letaxaban (TAK-442;TAK442)

Catalog No.: PC-63359Not For Human Use, Lab Use Only.

Letaxaban (TAK-442, TAK442) is a potent, selective and direct factor Xa (FXa) inhibitor with Ki of 1.8 nM for hFXa, >440-fold selectivity than thrombin and negligible effects on trypsin, plasmin, and tPA.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Letaxaban (TAK-442, TAK442) is a potent, selective and direct factor Xa (FXa) inhibitor with Ki of 1.8 nM for hFXa, >440-fold selectivity than thrombin and negligible effects on trypsin, plasmin, and tPA; In human plasma, TAK-442 doubles FXa-induced clotting time, prothrombin time (PT), and activated partial thromboplastin time at 0.19, 0.55, and 0.59 uM, respectively; demonstrates antithrombotic effects in rabbit model of venous thrombosis.

Thrombosis

Phase 2 Discontinued

Physicochemical Properties

M.Wt 479.98
Formula C22H26ClN3O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-(1-(3-((6-chloronaphthalen-2-yl)sulfonyl)-2-hydroxypropanoyl)piperidin-4-yl)tetrahydropyrimidin-2(1H)-one

References

1. Kawamura M, et al. J Cardiovasc Pharmacol. 2010 Aug;56(2):156-61.

2. Konishi N, et al. Thromb Res. 2010 Aug;126(2):124-9.

3. Konishi N, et al. Thromb Haemost. 2010 Sep;104(3):504-13.

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