2. Signalwege
  3. Vitamin D Related/Nuclear Receptor
  4. VKOR

VKOR

Vitamin K Epoxide Reductase

Vitamin K epoxide reductase (VKOR) is an integral membrane protein that catalyzes the reduction of vitamin K 2,3‐epoxide and vitamin K to vitamin K hydroquinone, a cofactor required for the γ‐glutamyl carboxylation reaction. The membrane topology model shows that VKOR spans the endoplasmic reticulum membrane three times with its amino‐terminus residing in the lumen and the carboxyl‐terminus residing in the cytoplasm. Both the active site (cysteines 132 and 135) and the proposed Warfarin binding site (tyrosine 139) reside in the third transmembrane helix. VKOR is the target of the widely used anticoagulant Warfarin which is proposed to exert its action by binding to the oxidized form of VKOR preventing the reduction of the essential cysteines to its active form. VKOR uses two cysteines, the CXXC redox motif, as the active site for KO reduction[1][2].

VKOR Verwandte Produkte (7):

Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-14854
    Tecarfarin
    		Antagonist 98.65%
    Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
    Tecarfarin
  • HY-111186
    Flocoumafen
    		Inhibitor 99.35%
    Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects.
    Flocoumafen
  • HY-14854A
    Tecarfarin sodium
    		Inhibitor
    Tecarfarin (ATI-5923) sodium is an orally active VKOR inhibitor with an IC50 of 0.67 μM against VKORC1. Tecarfarin sodium blocks the post-translational modification of vitamin K-dependent coagulation factors II, VII, IX and X, reducing their levels and activities. Tecarfarin sodium prolongs prothrombin time, attenuates venous and arterial thrombosis, increases ear incision bleeding volume, and exerts reversible anticoagulant effects. Tecarfarin sodium is applicable to research related to arterial and venous thrombosis as well as other diseases requiring anticoagulation.
    Tecarfarin sodium
  • HY-111186R
    Flocoumafen (Standard)
    		Inhibitor
    Flocoumafen (Standard) is the analytical standard of Flocoumafen. This product is intended for research and analytical applications. Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects.
    Flocoumafen (Standard)
  • HY-134999
    10-Hydroxywarfarin
    		Inhibitor
    10-Hydroxywarfarin, a metabolite of (R)-(+)-Warfarin (HY-W015998 ), is a CYP2C9 and vitamin K epoxide reductase complex 1 (VKOR) inhibitor with IC50s of 1.6 µM and 80 ng/mL, respectively.
    10-Hydroxywarfarin
  • HY-14854R
    Tecarfarin (Standard)
    		Antagonist
    Tecarfarin (ATI-5923) (Standard) is the analytical standard of Tecarfarin. This product is intended for research and analytical applications. Tecarfarin is an orally active VKOR inhibitor with an IC50 of 0.67 μM against VKORC1. Tecarfarin blocks the post-translational modification of vitamin K-dependent coagulation factors II, VII, IX and X, reducing their levels and activities. Tecarfarin prolongs prothrombin time, attenuates venous and arterial thrombosis, increases ear incision bleeding volume, and exerts reversible anticoagulant effects. Tecarfarin is applicable to research related to arterial and venous thrombosis as well as other diseases requiring anticoagulation.
    Tecarfarin (Standard)
  • HY-14854S
    Tecarfarin-13C,d3
    		Antagonist
    Tecarfarin-13C,d3 (ATI-5923-13C,d3) is 13C labeled Tecarfarin. Tecarfarin is an orally active VKOR inhibitor with an IC50 of 0.67 μM against VKORC1. Tecarfarin blocks the post-translational modification of vitamin K-dependent coagulation factors II, VII, IX and X, reducing their levels and activities. Tecarfarin prolongs prothrombin time, attenuates venous and arterial thrombosis, increases ear incision bleeding volume, and exerts reversible anticoagulant effects. Tecarfarin is applicable to research related to arterial and venous thrombosis as well as other diseases requiring anticoagulation.
    Tecarfarin-<sup>13</sup>C,d<sub>3</sub>