1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Glucocorticoid Receptor MMP
  3. Flocoumafen

Flocoumafen  (Synonyms: WL 108366)

目录号: HY-111186
COA 产品使用指南

Flocoumafen (WL 108366) 是一种具有口服活性的维生素 K 环氧化物还原酶抑制剂,也是一个多靶点配体,包括前列腺素 F 合成酶、血清白蛋白、糖皮质激素受体 (Glucocorticoid Receptor)-2、基质金属蛋白酶 (MMP)-9。Flocoumafen 是第二代抗凝血灭鼠剂 (ARs),半衰期为 177.4 h,有致命的抗凝作用。

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Flocoumafen Chemical Structure

Flocoumafen Chemical Structure

CAS No. : 90035-08-8

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Other Forms of Flocoumafen:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3].

IC50 & Target

MMP-9

 

Glucocorticoid Receptor 2

 

体外研究
(In Vitro)

Flocoumafen 最佳复合物是前列腺素F合成酶和血清白蛋白 (结合亲和力 ≥14.0 kcal/mol),其次是糖皮质激素受体-2、基质金属蛋白酶-9、核受体 ROR-α 以及活化素受体类型-1,结合亲和力 ≥13.5 kcal/mol[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Flocoumafen (0.02-0.1 mg/kg,每周一次,14 周) 在大鼠肝脏中有残留物堆积,且无法被完全代谢,高剂量下出现抗凝毒性[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Fischer rats[3]
Dosage: 0.02 and 0.1 mg/kg; once a week; for 14 weeks
Administration: Oral
Result: Caused noticeable cell accumulation in the liver, with residuals increasing as the dose rises at low doses, while at high doses, it stabilized after a while. The lethal anticoagulant effected only occurs when the binding sites were saturated.
Showed about 30% of the cumulative dosage disappeared from the feces within 3 days after each administration at low doses,for high doses, this value ranges from 18% after the first dose to 59% after the tenth dose, and anticoagulant toxicity appeared after six weeks.
分子量

542.54

Formula

C33H25F3O4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
HY-111186
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