Dihydrotestosterone(DHT)

Catalog No.S4757 Synonyms: androstanolone, stanolone, 5α-DHT

Dihydrotestosterone(DHT) Chemical Structure

Molecular Weight(MW): 290.44

Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.

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Biological Activity

Description Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.
Targets
Androgen Receptor [1]
()
In vitro

In AR-positive bladder cancer UMUC3 and TCC-SUP cells, dihydrotestosterone (DHT) increased the expression of EGFR and ERBB2 both in mRNA and in protein levels. DHT additionally upregulated the levels of phosphorylation of EGFR (pEGFR) and its downstream proteins AKT (pAKT) and ERK1/2 (pERK), induced by EGF treatment, in AR-positive cells[1].

In vivo DHT-treated SOD1-G93A mice demonstrate ameliorated muscle atrophy and increased body weight, which is associated with stronger grip-strength. DHT treatment increases the expression of insulin-like growth factor-1 in muscle, which can exert myotrophic as well as neurotrophic effects through retrograde transport. DHT treatment attenuates neuromuscular junction denervation, and axonal and motoneuron loss. DHT-treated SOD1-G93A mice demonstrates improvement in motor behavior as assessed by rota-rod and gait analyses, and an increased lifespan[2].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Bladder cancer cells
  • Concentrations: 1 nM
  • Incubation Time: 24 h
  • Method:

    Bladder cancer cells at a density of 50-60% confluence in 24-well plates are co-transfected with 250 ng of MMTV-luc reporter plasmid DNA and 2.5 ng of PRL-TK-luc plasmid DNA. After 6 h of transfection, the medium is replaced with another medium supplemented with charcoal-stripped FBS in the presence or absence of ligands (DHT, HF, or both) for 24 h. Cells were harvested, lysed, and assayed for luciferase activity.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: SOD1-G93A mutant mice with the congenic C57BL/6J background
  • Formulation: saline
  • Dosages: 5 mg
  • Administration: silastic implant
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 58 mg/mL (199.69 mM)
Ethanol 58 mg/mL (199.69 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 290.44
Formula

C19H30O2

CAS No. 521-18-6
Storage powder
in solvent
Synonyms androstanolone, stanolone, 5α-DHT

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02697032 Recruiting Breast Cancer University Medical Center Groningen February 2016 Phase 2
NCT01724619 Terminated Prostate Cancer Wake Forest University Health Sciences November 2012 Early Phase 1
NCT00490022 Completed Healthy University of Washington|National Institute on Aging (NIA)|ASCEND Therapeutics June 2007 Phase 1|Phase 2
NCT00163566 Unknown status Hypogonadism|Late Onset Hypogonadism|Low Testosterone ASCEND Therapeutics October 2004 Phase 2

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID