Bexlosteride.

Names

[ Name ]:
Bexlosteride.

[Synonym ]:
Benzo[f]quinolin-3(2H)-one, 8-chloro-1,4,4a,5,6,10b-hexahydro-4-methyl-, (4aR,10bR)-
(4aR,10bR)-8-Chloro-4-methyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
36X732P4P0
bexlostéride
(4aR-trans)-8-Chloro-4-methyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
Benzo(f)quinolin-3(2H)-one, 8-chloro-1,4,4a,5,6,10b-hexahydro-4-methyl-, trans-
Bexlosteride

Biological Activity

[Description]:

Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

[Target]

human type I 5α-reductase[1]

[In Vitro]

Bexlosteride concentration-dependently inhibits reductive metabolism of [3H-T] in the LNCaP cells, with an IC50 of 5.77 nM[1]. Bexlosteride significantly antagonizes Testosterone-induced stimulation of LNCaP cellular proliferation at concentrations greater than 10 nM, and at 1000 nM completely blocks the mitogenic effects of Testosterone on LNCaP cells[1]. Bexlosteride significantly antagonizes Testosterone -induced PSA secretion at a concentration equal to or greater than 30 nM[1].

[References]

[1]. Sutkowski DM, et, al. Responses of LNCaP prostatic adenocarcinoma cell cultures to LY300502, a benzoquinolinone human type I 5alpha-reductase inhibitor. Prostate Suppl. 1996;6:62-6.

[2]. 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 Oct;24(10):1162-5.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
413.9±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₆ClNO

[ Molecular Weight ]:
249.736

[ Flash Point ]:
204.1±28.7 °C

[ Exact Mass ]:
249.092041

[ LogP ]:
3.17

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.571

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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