Bexlosteride(Synonyms: LY300502)

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Bexlosteride (Synonyms: LY300502)

Bexlosteride (LY300502) 是一种人类 I 型 5α-还原酶抑制剂。Bexlosteride 在 LNCaP 细胞培养物中显示出代谢抑制、抗增殖和抗分泌作用。Bexlosteride 可用于前列腺癌的研究。

Bexlosteride(Synonyms: LY300502)

Bexlosteride Chemical Structure

CAS No. : 148905-78-6

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生物活性

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].

IC50 & Target

human type I 5α-reductase[1]

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

249.74

Formula

C14H16ClNO

CAS 号

148905-78-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [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.

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