LY191704 

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].

Human Type I 5α-Reductase^[1][2]

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 K_i 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.

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.

249.74

C₁₄H₁₆ClNO

146117-78-4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Farid NA, et al. Stereoselective disposition of the enantiomers of the benzoquinolinone LY191704, a human type I 5 alpha-reductase inhibitor. Differences between rats and dogs. Drug Metab Dispos. 1996;24(10):1162-1165.  [Content Brief]

  [2]. Hirsch KS, et al. LY191704: a selective, nonsteroidal inhibitor of human steroid 5 alpha-reductase type 1. Proc Natl Acad Sci U S A. 1993;90(11):5277-5281.  [Content Brief]