1. Metabolic Enzyme/Protease
  2. 5 alpha Reductase
  3. LY191704

LY191704 作为一种苯并喹啉酮,是一种高效、非甾体、非竞争性和选择性 human type I 5α-reductase 抑制剂。LY191704 是 LY300502 和 LY300503 化合物的外消旋混合物。LY191704 可能有助于研究由 human type I 5α-reductase 产生的二氢睾酮 (DHT) 过多引起的人类内分泌紊乱。

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LY191704 Chemical Structure

LY191704 Chemical Structure

CAS No. : 146117-78-4

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Other Forms of LY191704:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1[1][2].

IC50 & Target

Human Type I 5α-Reductase[1][2]

体外研究
(In Vitro)

LY191704 (0.001-100 uM) inhibits the conversion of testosterone to DHT with an IC50 of 10 nM in Hs68 cells. LY191704 inhibits the enzyme expressed by the human cells with an IC50 of 12 nM but is virtually inactive against the 5α-reductase expressed by rat prostate cells. LY191704 is a potent and specific inhibitor of human 5α-reductase type 1 but had little or no activity against human 5α-reductase type 2 or rat 5α-reductase type 1. A Ki value of 17.1 μM is determined for the human type 2 enzyme, indicating that LY191704 demonstrates an 5000-fold selectivity for the human type 1 isozyme[2].

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

体内研究
(In Vivo)

LY191704 (10, 30, or 100 mg/kg; p.o.; 1 month) increases plasma concentrations[1].

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

Animal Model: Rats[1]
Dosage: 10, 30, or 100 mg/kg
Administration: P.o.; 1 month
Result: Increased plasma concentrations.
分子量

249.74

Formula

C14H16ClNO

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:
LY191704
目录号:
HY-118091
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