GHSR Human Ghrelin GPCR Cell Based Antagonist Calcium Flux LeadHunter Assay - FR

Item: 1657

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

The receptor for GHS (GHS-R) is a member of the superfamily of G-protein-coupled receptors. Ghrelin, an endogenous 28 amino acid present in the stomach, acts as a specific endogenous ligand for the GHS-R. Ghrelin has demonstrated potent and reproducible GH-releasing activity as well as significant prolactin-, ACTH- and cortisol-releasing activity. Its major physiological function may relate to energy homeostasis.

Family:

GPCR

Sub Family:

Ghrelin

Class:

Class A

Protein Name:

GHSR

Uniprot Number:

Q92847

Protein Aliases:

GH-releasing peptide receptor|GHRP|Ghrelin receptor

Gene Name:

GHSR

Gene ID:

2693

Accession Number:

NM_004122

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

22°C

Control Inhibitor:

[D-Arg1,D-Phe5,D-Trp7,9,D-Leu11]-SP

Control Activator:

ghrelin (3 nM)

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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

Name

[D-Arg1,D-Phe5,D-Trp7,9,D-Leu11]-SP

Measurement

88nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

In man, ghrelin was shown to stimulate food intake; it may also increase weight gain by reducing fat utilization.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault