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].
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VKOR Verwandte Produkte (11)
Verwandte Produkte (11)
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Anisindione
0 ImagesAnisindione is an anticoagulant, a GGCX inhibitor, and a VKORC1 inhibitor. Anisindione directly occupies the vitamin K binding pocket of γ-glutamyl carboxylase (GGCX) and acts as a competitive antagonist of GGCX. Anisindione reduces plasma prothrombin activity. The effect of Anisindione can be interrupted by phytonadione, and it lacks hepatobiliary or hematological toxicity, making it useful for research on thrombosis, deep vein thrombosis, and pulmonary embolism.
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(R)-(+)-Warfarin
0 Images(R)-(+)-Warfarin is an orally active chiral 4-hydroxycoumarin compound with vitamin K epoxide reductase (VKOR) inhibitory activity and cytochrome P450 substrate activity. (R)-(+)-Warfarin undergoes stereoselective metabolism via CYP1A2 to form 6-Hydroxywarfarin and 8-Hydroxywarfarin, and is metabolized via CYP3A4 to produce 10-Hydroxywarfarin (HY-134999). (R)-(+)-Warfarin can be used for the research of thromboembolic diseases.
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Flocoumafen
0 ImagesSynonyms: WL 108366Flocoumafen (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.
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(R)-(+)-Warfarin-d5
0 Images(R)-(+)-Warfarin-d5 is the deuterated-labeled (R)-(+)-Warfarin (HY-W015998). (R)-(+)-Warfarin is an orally active chiral 4-hydroxycoumarin compound with vitamin K epoxide reductase (VKOR) inhibitory activity and cytochrome P450 substrate activity. (R)-(+)-Warfarin undergoes stereoselective metabolism via CYP1A2 to form 6-Hydroxywarfarin and 8-Hydroxywarfarin, and is metabolized via CYP3A4 to produce 10-Hydroxywarfarin (HY-134999). (R)-(+)-Warfarin can be used for the research of thromboembolic diseases.
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Tecarfarin sodium
0 ImagesArt. -Nr.: HY-14854ACAS. Nr.: 1004551-83-0Synonyms: ATI-5923 sodiumTecarfarin (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.
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Flocoumafen (Standard)
0 ImagesArt. -Nr.: HY-111186RCAS. Nr.: 90035-08-8Synonyms: WL 108366 (Standard)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.
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10-Hydroxywarfarin
0 Images10-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.
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Anisindione (Standard)
0 ImagesAnisindione (Standard) is the analytical standard of Anisindione (HY-B0924). This product is intended for research and analytical applications. Anisindione is an anticoagulant, a GGCX inhibitor, and a VKORC1 inhibitor. Anisindione directly occupies the vitamin K binding pocket of γ-glutamyl carboxylase (GGCX) and acts as a competitive antagonist of GGCX. Anisindione reduces plasma prothrombin activity. The effect of Anisindione can be interrupted by phytonadione, and it lacks hepatobiliary or hematological toxicity, making it useful for research on thrombosis, deep vein thrombosis, and pulmonary embolism.
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Tecarfarin (Standard)
0 ImagesSynonyms: ATI-5923 (Standard)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.
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Tecarfarin-13C,d3
0 ImagesArt. -Nr.: HY-14854SSynonyms: ATI-5923-13C,d3Tecarfarin-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.
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