Finasteride

Catalog No.S1197 Synonyms: MK-906

Finasteride Chemical Structure

Molecular Weight(MW): 372.54

Finasteride is a potent, reversible inhibitor of the rat type 1 5 alpha-reductase with Ki of 10.2 nM, used in the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB).

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Biological Activity

Description Finasteride is a potent, reversible inhibitor of the rat type 1 5 alpha-reductase with Ki of 10.2 nM, used in the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB).
Targets
5-α reductase [1]
10.2 nM(Ki)
In vitro

Finasteride binds to the type 2 isozyme-NADPH complex to form a ternary complex with Ki of 1.19 nM, which then rearranges to a high affinity complex (E:I) with a pseudo first order rate constant of 1.62 ms. [1] Finasteride dose-dependently inhibits the growth rate of the LnCap cell line. [2] Finasteride markedly inhibits prostate-specific antigen (PSA) secretion and expression in LNCaP cells. [3]

In vivo Finasteride induces dosage-related incidences of hypospadias (penischisis) in male offspring with a threshold dosage level near 0.1 mg/kg/day and a 100% effect level of 100 mg/kg/day in male rats. Finasteride also causes decreased anogenital distance in male offspring in male rats. [4] Finasteride and castration decreases prostate weight at day 21 by 65% and 93%, respectively, in rats. Finasteride has no significant effect on DNA content after 4 days and decreases DNA content by a maximum of 52% at 14 days in rats. Finasteride causes a less intense increase in staining in which 16% of epithelial cells stained for tissue transglutaminase on day 9 with a return to baseline by day 14 in rats. Finasteride-induced staining is less intense with peak staining at day 4 (0.7% of epithelial cells) and a return to control values by day 9 in rats. [5]

Protocol

Solubility (25°C)

In vitro DMSO 75 mg/mL (201.32 mM)
Ethanol 75 mg/mL (201.32 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 372.54
Formula

C23H36N2O2

CAS No. 98319-26-7
Storage powder
Synonyms MK-906

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02483195 Withdrawn Female Androgenetic Alopecia University of Florida August 2016 Phase 4
NCT03004469 Recruiting Alopecia, Androgenetic Polichem S.A. July 2016 Phase 3
NCT02781311 Recruiting Alopecia Allergan June 2016 Phase 2
NCT02791243 Completed Androgenetic Alopecia Polichem S.A. April 2016 Phase 1
NCT02548117 Withdrawn ERYTHROCYTOSIS Baylor College of Medicine February 2016 Phase 3
NCT02502669 Recruiting NODULOCYSTIC ACNE Elorac, Inc. July 2015 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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5-alpha Reductase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID