| Bioactivity | 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]. |
| Target | human type I 5α-reductase |
| Invitro | 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]. |
| Name | Bexlosteride |
| CAS | 148905-78-6 |
| Formula | C14H16ClNO |
| Molar Mass | 249.74 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |