Biological Information
Background Information:
Estrogens, produced by ovaries and testis, affect growth and differentiation of many target tissues. These include the male and female reproductive tissues (mammary gland, uterus, ovary, and prostate). Estrogens have also been implicated in the physiology of the bone, cardiovascular tissues, and the brain. Two distinct estrogen receptors (ERα and ERß) bind estrogen as well as other agonists and antagonists. Estrogen receptor is a member of the super family of nuclear receptor that show a similar structure and mode of action.
Family:
NHR
Sub Family:
Estrogen
Class:
Steroid
Protein Name:
ERalpha
Uniprot Number:
P03372
Protein Aliases:
ER-alpha|Estradiol receptor|Nuclear receptor subfamily 3 group A member 1
Gene Name:
ESR1
Gene ID:
2099
Gene Aliases:
NR3A1|Era
Accession Number:
NM_001328100
Organism:
Human
Construct Details:
LBD, Recombinant
Assay Information
Assay Type:
Functional
Assay Sub Type:
Protein-Protein Interaction
Functional Mode:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
10 min at RT
Control Inhibitor:
Fulvestrant
Criteria For Significance:
≥ 50% decrease in fluorescence relative to estriol response, ≥ 50% Increase in fluorescence relative to estriol 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:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Adverse / Beneficial Action:
Estrogen antagonists may be useful in improving the treatment of menopause and breast cancers.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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