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].

References:

[1]. Tie JK, et al. Structure and function of vitamin K epoxide reductase. Vitam Horm. 2008;78:103-30. [Content Brief]

[2]. Sinhadri BCS, et al. Vitamin K epoxide reductase and its paralogous enzyme have different structures and functions. Sci Rep. 2017 Dec 15;7(1):17632. [Content Brief]

VKOR Related Products (6):

By Effects:	Inhibitors (4) Antagonists (2)

Cat. No.	Product Name	Effect	Purity	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 .

HY-111186

Flocoumafen	Inhibitor	99.17%
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.

HY-14854A

Tecarfarin sodium	Inhibitor
Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin sodium has the antithrombotic activity.

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.

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.

HY-14854S

Tecarfarin-¹³C,d₃	Antagonist
Tecarfarin-¹³C,d₃ (ATI-5923-¹³C,d₃) is ¹³C labeled Tecarfarin. 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 .

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