AR Human Androgen NHR Cell Based Agonist Reporter LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Androgen receptor (AR) is the member of steroid nuclear hormone receptors family that is activated by binding a diverse array of the small, hydrophobic ligands including steroid hormones in the cytoplasm and then translocating into the nucleus to regulate target gene transcription. AR signaling may be involved in development of prostate cancer. Androgen receptor reporter is a cell-based functional assay to measure the transcriptional ability of androgen receptor in response to testing substance.
Family:
NHR
Sub Family:
3-Ketosteroid
Class:
Steroid
Protein Name:
AR
Uniprot Number:
P10275
Protein Aliases:
testicular feminization|Kennedy disease
Gene Name:
AR
Gene ID:
367
Gene Aliases:
AIS|NR3C4|SMAX1|HUMARA
Accession Number:
BC132975.1
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
Luminescence/spectrofluorimetry
Measured Response:
Luminescence/Fluorescence
Testing Information
Procedure Summary:
CHO-K1-hAR clone F9 cells expressing human full-length AR are transfected with an MMTV LTR (Murine Mammary Tumor Virus Long Terminal Repeat)-driven luciferase reporter plasmid and seeded overnight. Test compound or vehicle is incubated with the cells at 37°C, 5% CO₂ for 18 hours. AR reporter activity is evaluated by a luciferase assay and normalized to a viability assay. Luminescence and fluorescence signals from the luciferase and viability assay, respectively, are measured using a microplate reader. Test compound-induced luminescence-to-fluorescence ratio induction by 50 percent or more (≥50%) relative to 100 nM 5α-dihydrotestosterone response indicates possible AR agonist activity. Test compound-induced inhibition of the 300 pM 5α-dihydrotestosterone-induced luminescence-to-fluorescence ratio by 50 percent or more (≥50%) indicates possible AR antagonist activity.
Incubation:
18 hr at 37°C
Control Activator:
5α-Dihydrotestosterone
Criteria For Significance:
≥ 50% increase in luminescence relative to dihydrotestosterone response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Adverse / Beneficial Action:
Testosterone receptor agonists may promote prostate cancer and cause edema while antagonists may inhibit spermatogenesis and be useful in the treatment of prostate cancer.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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