Home Endocrinology & Hormones 5-alpha Reductase inhibitor Dutasteride For research use only.

Dutasteride

Synonyms: GI198745, GG-745

Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).

Dutasteride Chemical Structure

Dutasteride Chemical Structure

CAS: 164656-23-9

Selleck's Dutasteride has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Biological Activity

Description Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).
Targets
5-α reductase [1]
In vitro
In vitro

Dutasteride inhibits type-1 5AR and type-2 5AR with IC50 of 6 nM and 7 nM, respectively. Dutasteride is 60-fold more potent than Finasteride in its initial Ki versus type 1 5AR and ~5-fold more rapid in inactivating the enzyme. [1]

Dutasteride inhibits (3)H-T conversion to (3)H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation in LNCaP cells. Dutasteride also inhibits DHT-induced PSA secretion and cell proliferation with IC50 of 1 μM in LNCaP cells. Dutasteride competes for binding the LNCaP cell AR with an IC50 of 1.5 μM. Dutasteride (10–50 μM) results in enhanced cell death, possibly by apoptosis, in steroid-free medium. [2]

Dutasteride reduces cell viability and cell proliferation in androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer(PCa) cell lines. Dutasteride results in overexpressed genes included genes encoding for proteins involved in biosynthesis and metabolism of androgen (HSD17B1;HSD17B3;CYP11B2), androgen receptor and androgen receptor co-regulators (AR;CCND1), and signal transduction(ERBB2; V-CAM; SOS1) whereas, underexpressed genes (KLK3; KLK2; DHCR24) are androgen-regulated genes (ARGs) in androgen-responsive (LNCaP) cell. [3]

Dutasteride inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells. [4]
Cell Research Cell lines LNCaP Cells
Concentrations 1 μM
Incubation Time 5 days
Method

Cells were treated with various concentrations of drug for 5 days.
In Vivo
In vivo

Dutasteride (100 mg/kg/day) has prostates about half as large as those in intact male rats treated with vehicle alone. Dutasteride is orally bioavailable and because of its mechanism of action it easily overcomes the potential liability of being >99% plasma protein bound. [1]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 0.5 mg/kg
Administration i.g. gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03669692 Withdrawn Prostatic Hyperplasia Benign|Metabolic Syndrome Complexo Hospitalario Universitario de A Coruña July 10 2018 Not Applicable
NCT02839122 Completed Benign Prostate Hyperplasia Yuyu Pharma Inc. May 2016 Phase 1
NCT02352311 Completed Benign Prostate Hyperplasia|Healthy Dongkook Pharmaceutical Co. Ltd. January 2015 Phase 1

Chemical lnformation & Solubility

Molecular Weight 528.53 Formula

C27H30F6N2O2
CAS No. 164656-23-9 SDF Download Dutasteride SDF
Smiles CC12CCC3C(C1CCC2C(=O)NC4=C(C=CC(=C4)C(F)(F)F)C(F)(F)F)CCC5C3(C=CC(=O)N5)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 106 mg/mL ( (200.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


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In vivo
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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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