vkor

Tecarfarin sodium is a novel orally active non-competitive vitamin K epoxide reductase antagonist. Tecarfarin sodium has the antithrombotic activity.

Tecarfarin (ATI-5923) 是一种具有口服活性和有效性的维生素 K 环氧化物还原酶 (VKOR) 拮抗剂和大麻素-1受体反向激动剂，具有抗血栓形成活性，可减轻小鼠的腹痛并增加肠道转运。

Phenindione (Rectadione) 是一种茚满二酮，已被用作抗凝剂，可作为维生素 K 拮抗剂。它的作用类似于华法林，但由于其严重不良反应的发生率较高，现在很少使用。

Warfarin sodium 是一种抗凝血剂，通过抑制维生素 K 依赖性凝血因子的合成起作用。华法林适用于预防和 或治疗静脉血栓形成及其延伸、肺栓塞和房颤栓塞。它还用作预防心肌梗塞后全身性栓塞的辅助剂。华法林也用作杀鼠剂。

10-hydroxy Warfarin is a metabolite of (R)-warfarin .1It is formed from (R)-warfarin by the cytochrome P450 (CYP) isoform CYP3A4. 10-hydroxy Warfarin is an inhibitor of CYP2C9 (IC50= 1.6 μM), the enzyme that converts (S)-warfarin to its 6-hydroxy warfarin and 7-hydroxy warfarin metabolites.2 1.Kaminsky, L.S., and Zhang, Z.-Y.Human P450 metabolism of warfarinPharmacol. Ther.73(1)67-74(1997) 2.Jones, D.R., Kim, S.-Y., Guderyon, M., et al.Hydroxywarfarin metabolites potently inhibit CYP2C9 metabolism of S-warfarinChem. Res. Toxicol.23(5)939-945(2010)