1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
  3. FPL 66564

FPL 66564 是一种短效血管紧张素转换酶 (ACE) 抑制剂,对兔 ACEIC50 为 5.7 nM。FPL 66564 可在功能层面抑制 ACE 活性,且会被人血水解切割为无活性的亲水性代谢产物。FPL 66564 可调节麻醉大鼠中血管紧张素 I 诱导的升压反应,在停止静脉输注后其作用会迅速消退至基线水平。FPL 66564 可用于危重症相关心血管调控的研究。

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FPL 66564

FPL 66564 Chemical Structure

CAS No. : 140369-78-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FPL 66564 is a short-acting angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 5.7 nM against rabbit ACE. FPL 66564 inhibits ACE activity at the functional level and is hydrolyzed in human blood into inactive hydrophilic metabolites. FPL 66564 modulates angiotensin I-induced pressor responses in anesthetized rats, and its effects rapidly return to baseline after cessation of intravenous infusion. FPL 66564 can be used for research on cardiovascular regulation related to critical illness[1][2].

IC50 & Target[1]

ACE

5.7 nM (IC50)

体外研究
(In Vitro)

FPL 66564 在人血中发生降解,半衰期为 14 分钟,生成无活性的亲水性小分子产物[2]

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

体内研究
(In Vivo)

FPL 66564 (100-1000 nmoL/kg/min;静脉注射;持续输注) 可在氨基甲酸乙酯麻醉大鼠中快速实现对血管紧张素 I 升压反应的持续性、剂量依赖性抑制,且输注停止后其作用会迅速消失[2]

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

Animal Model: Rat (anesthetized with urethane)[2]
Dosage: 100 nmol/kg/min; 300 nmol/kg/min; 1000 nmol/kg/min
Administration: i.v.; continuous infusion
Result: Achieved rapid equilibrium of pressor response inhibition, followed by a sustained plateau.
Maintained ~90-95% inhibition of pressor response during infusion at 1000 nmol/kg/min dose.
Maintained ~75-80% inhibition during infusion at 300 nmol/kg/min dose.
Maintained ~60-65% inhibition during infusion at 100 nmol/kg/min dose.
Rapidly dissipated inhibitory effect on cessation of infusion, with all groups returning to near-baseline levels of inhibition (≤25%) by 60 minutes post-infusion.
分子量

238.32

Formula

C8H14O4S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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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产品名称:
FPL 66564
目录号:
HY-182445
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