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

PubChem ID

104741

Name

ICI182780

Measurement

4.8nM - IC50

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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