Description
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.
Product information
CAS Number: 146117-78-4
Molecular Weight: 249.74
Formula: C14H16ClNO
Chemical Name: (4aR, 10bR)-8-chloro-4-methyl-1H, 2H, 3H, 4H, 4aH, 5H, 6H, 10bH-benzo[f]quinolin-3-one, rel
Smiles: CN1[C@@H]2CCC3=CC(Cl)=CC=C3[C@H]2CCC1=O |&1:2,12,r|
InChiKey: WQBIOEFDDDEARX-NYZMZBMTNA-N
InChi: InChI=1/C14H16ClNO/c1-16-13-6-2-9-8-10(15)3-4-11(9)12(13)5-7-14(16)17/h3-4,8,12-13H,2,5-7H2,1H3/t12-,13-/s3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
In Vivo:
LY191704 (10, 30, or 100 mg/kg; p.o.; 1 month) increases plasma concentrations.
Products are for research use only. Not for human use.
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