Bexlosteride  (Synonyms: LY300502)

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].

human type I 5α-reductase^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

249.74

C₁₄H₁₆ClNO

148905-78-6

CN1[C@@]2([H])[C@@](CCC1=O)([H])C3=CC=C(Cl)C=C3CC2

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [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.  [Content Brief]