Bexlosteride
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.
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- CAS No.: 148905-78-6
- Formule: C14H16ClNO
- Masse moléculaire:249.74
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 148905-78-6
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Masse moléculaire 249.74
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Formule C14H16ClNO
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SMILES
CN1[C@@]2([H])[C@@](CCC1=O)([H])C3=CC=C(Cl)C=C3CC2
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Synonyms
LY300502
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bexlosteride Related Classifications
HY-118091A Related Classifications
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