146117-78-4
146117-78-4 structure
- Name: LY191704
- Chemical Name: (4aS,10bS)-8-chloro-4-methyl-1,2,4a,5,6,10b-hexahydrobenzo[f]quinolin-3-one
- CAS Number: 146117-78-4
- Molecular Formula: C14H16ClNO
- Molecular Weight: 249.73600
- Catalog: Signaling Pathways Metabolic Enzyme/Protease 5 alpha Reductase
- Create Date: 2017-04-25 15:33:06
- Modify Date: 2024-01-10 16:16:40
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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].
| Name | (4aS,10bS)-8-chloro-4-methyl-1,2,4a,5,6,10b-hexahydrobenzo[f]quinolin-3-one |
|---|---|
| Synonyms |
8-Chloro-4-methyl-1,2,3,4,4a,5,6,10b-octahydrobenzo(f)quinolin-3(2H)-one
Benzo(f)quinolin-3(2H)-one,8-chloro-1,4,4a,5,6,10b-hexahydro-4-methyl-,trans |
| 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[1][2]. |
|---|---|
| Related Catalog | |
| Target |
Human Type I 5α-Reductase[1][2] |
| 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]. |
| In Vivo | LY191704 (10, 30, or 100 mg/kg; p.o.; 1 month) increases plasma concentrations[1]. Animal Model: Rats[1] Dosage: 10, 30, or 100 mg/kg Administration: P.o.; 1 month Result: Increased plasma concentrations. |
| References |
| Molecular Formula | C14H16ClNO |
|---|---|
| Molecular Weight | 249.73600 |
| Exact Mass | 249.09200 |
| PSA | 20.31000 |
| LogP | 2.92850 |
| Vapour Pressure | 4.65E-07mmHg at 25°C |