Biological Information

Background Information:

The gonadotropin- The Gonadotropin-releasing hormone receptor (GNRHR), also known as leutinizing hormone releasing hormone receptor (LHRHR), is a member of the seven-transmembrane G-Protein coupled receptor (GPCR) family. It is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary and prostate. GnRH (Gonadotropin-releasing hormone ), a decapeptide produced by the hypothalamus, plays an important role in the reproduction by regulating the pituitary-gonadal axis. Continuous high doses of GnRH or its super active agonists result in desensitization of the pituitary gonadotropes and a suppression of sex steroid production by the gonads (chemical castration). Based on these effects, the treatments with GnRH agonists has become widely used hormonal therapy of sex-steroid dependent tumors. It was also demonstrated that most tumor cells contain GnRH receptors, and the direct antiproliferative effects of GnRH analogs on cancer cells might be mediated through these receptors.

Family:

GPCR

Sub Family:

Gonadotrophin-Releasing Hormone

Class:

Class A

Protein Name:

GnRH

Uniprot Number:

P30968

Protein Aliases:

GnRH-R

Gene Name:

GNRHR

Gene ID:

2798

Gene Aliases:

LHRHR

Accession Number:

NM_000406

Organism:

Human

Construct Details:

Recombinant

Cell Type:

Chem-1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

Cetrorelix

Control Activator:

LHRH (3 nM)

Test Concentration / Dose:

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

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

25078429

Name

Cetrorelix

Measurement

3nM - IC50

Clinical Relevance

Adverse / Beneficial Action:

GnRH agonists are developed and utilized as anti-cancer agents.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 4268
Item: G274