产品
编 号：F690122
分子式：C14H16ClNO
分子量：249.74
分子式：C14H16ClNO
分子量：249.74
产品类型
规格
价格
是否有货
结构图
CAS No: 146117-78-4
产品详情
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.
体内研究：
LY191704 (10, 30, or 100 mg/kg; p.o.; 1 month) increases plasma concentrations.Animal Model:Rats
Dosage:10, 30, or 100 mg/kg
Administration:P.o.; 1 month
Result:Increased plasma concentrations.
体外研究：
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.
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.
体内研究：
LY191704 (10, 30, or 100 mg/kg; p.o.; 1 month) increases plasma concentrations.Animal Model:Rats
Dosage:10, 30, or 100 mg/kg
Administration:P.o.; 1 month
Result:Increased plasma concentrations.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备