ERalpha Human Estrogen NHR Binding Agonist Radioligand LeadHunter Assay - FR

Item: 5484

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Status: Available

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OVERVIEW

DOCUMENTS/REFERENCES

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

Gene Name:

ESR1

Gene ID:

2099

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Testing Information

Ligand:

[3H] Estradiol

Ligand Kd (nM):

0.26 nM

Ligand Concentration:

0.4 nM

Non Specific:

Diethylstilbestrol (1 µM)

Incubation:

120 min at 22°C

Test Sample Requirements:

Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5757

Name

Estradiol

Measurement

0.36nM - IC50

PubChem ID

5991

Name

Ethinyl estradiol

Measurement

0.35nM - IC50

PubChem ID

448537

Name

Diethylstilbestrol

Measurement

0.33nM - IC50

PubChem ID

2733526

Name

Tamoxifen

Measurement

3.46nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

Estrogen receptor agonists may alter the menstrual cycle, prevent conception, decrease bone resorption and increase risk of breast cancer in females while antagonists may alter the menstrual cycle and be useful in the treatment of breast cancer.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault