247131-06-2
Chemical Structure
JTV-803
- CAS No.: 247131-06-2
- Formula:C22H27N5O3
- Molecular Weight:409.48
InChIKey: MISBTXJXWSXZBF-UHFFFAOYSA-N
SMILES: O=C(C1(CCN(CC1)C2=CC=NC=C2)COC3=CC=C4C(CN(CC4)C(N)=N)=C3)O
Biological Activity: JTV-803 is a selective and competitive direct factor Xa (FXa) inhibitor with a Ki of 19 nM and an IC50 of 81 nM against human FXa, and its action is independent of antithrombin III (ATIII). JTV-803 exhibits significantly higher selectivity for human FXa than for thrombin, plasmin, and trypsin. JTV-803 produces sustained ex vivo anti-FXa inhibitory activity in vivo. JTV-803 prolongs aPTT and PT, prevents dialyzer thrombosis, and is cleared during dialysis. JTV-803 dose-dependently attenuates coagulation activation, maintains plasma ATIII activity, reduces glomerular fibrin deposition, and improves survival rate. JTV-803 can be used for research related to thrombosis and hemodialysis anticoagulation[1][2][3].
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JTV-803 | JTV-803 is a selective and competitive direct factor Xa (FXa) inhibitor with a Ki of 19 nM and an IC50 of 81 nM against human FXa, and its action is independent of antithrombin III (ATIII). JTV-803 exhibits significantly higher selectivity for human FXa than for thrombin, plasmin, and trypsin. JTV-803 produces sustained ex vivo anti-FXa inhibitory activity in vivo. JTV-803 prolongs aPTT and PT, prevents dialyzer thrombosis, and is cleared during dialysis. JTV-803 dose-dependently attenuates coagulation activation, maintains plasma ATIII activity, reduces glomerular fibrin deposition, and improves survival rate. JTV-803 can be used for research related to thrombosis and hemodialysis anticoagulation. | |||||||||||||||||||||
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References
- [1]. Hayashi M, et al. Inhibitory effect of JTV-803, a new cyclic guanidine derivative, on factor Xa in vitro and in vivo. European journal of pharmacology. 2001 Oct 05;428(2):163-8.
- [2]. Hayashi M, et al. Effects of activated factor X inhibitor, JTV-803, in a pig model of hemodialysis. Thrombosis research. 2002 Sep 15;107(6):351-6.
- [3]. Asakura H, et al. Beneficial effect of JTV-803, a new synthetic inhibitor of activated factor X, against both lipopolysaccharide-induced and tissue factor-induced disseminated intravascular coagulation in rat models. Blood Coagul Fibrinolysis. 2002 Apr;13(3):233-9.
