GR Human Glucocorticoid NHR Binding Agonist Radioligand LeadHunter Assay - FR

Item: 469

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Glucocorticoid receptors are members of a superfamily of nuclear receptors that transduce the effects of a diverse array of small, hydrophobic ligands, including the steroid hormones, thyroid hormone, vitamin D and retinoids. Potencies for glucocorticoid receptor activation upon glucose metabolism closely parallel those for antiinflammatory effects.

Family:

NHR

Sub Family:

3-Ketosteroid

Class:

Steroid

Protein Name:

Uniprot Number:

P04150

Protein Aliases:

glucocorticoid receptor

Gene Name:

NR3C1

Gene ID:

2908

Gene Aliases:

GR|GRL

Accession Number:

XM_005268419

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]dexamethasone

Ligand Kd (nM):

1.5

Ligand Concentration:

1.5 nM

Non Specific:

10 µM Triamcinolone

Incubation:

24h at 4°C

Control Inhibitor:

Dexamethazone

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

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

5994

Name

Progesterone

Measurement

69nM - IC50

PubChem ID

24278426

Name

17-beta -estradiol

Measurement

1736nM - IC50

PubChem ID

24893536

Name

Dexamethazone

Measurement

3nM - IC50

PubChem ID

329826845

Name

Traimcinolone

Measurement

1.8nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Glucocorticoid receptor agonists are immunosuppressive and antiinflammatory; prolonged administration may cause hypertension, hyperglycemia, osteoporosis, susceptibility to infection.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault