CGRP (CLR/RAMP1) Human Calcitonin GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

The calcitonin family of bioactive peptides comprises of calcitonin, amylin, two calcitonin-gene related peptides (CGRP1, and CGRP2) and adrenomedullin. Adrenomedullin is a 52-aa hypotensive peptide. It has structural similarity with CGRP and amylin. ADM is produced in peripheral tissues, adrenal medulla, lung, and kidney. Co-expression of receptor activity modifying protein RAMP2 and RAMP3 with calcitonin receptor-like receptor (CRLR) has been identified respectively as the adrenomedullin receptor 1 (AMR1) designated the CRLR/RAMP2 receptor and the adrenomedullin receptor 2 (AMR2) denoted as the CRLR/RAMP3 receptor. The three known RAMP isoforms (1-3) have been identified as distinct gene products and are required for receptor plasma membrane expression as well as for determination of CRLR receptor phenotype and specificity. Adrenomedullin receptors are coupled to the Gs protein resulting in elevation of intracellular cAMP, Ca2+ mobilization and nitric oxide production. Adrenomedullin receptor agonism may result in hypotension associated with cardiac inotropic activity, angiogenesis and mitogenic activity promoting human malignancies. Adrenomedullin receptor antagonism may find therapeutic use in the treatment of heart disease, cerebral vascular disease, type I diabetes and immune disorder, sepsis and cancer.

Family:

GPCR

Sub Family:

Calcitonin

Class:

Class B

Protein Name:

CLR

Uniprot Number:

Q16602

Protein Aliases:

Calcitonin receptor-like receptor

Gene Name:

CALCRL

Gene ID:

10203

Gene Aliases:

CGRPR|CRLR

Accession Number:

NM_005795

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]hCGRPalpha

Ligand Kd (nM):

0.06

Ligand Concentration:

0.03 nM

Non Specific:

1 µM HCGRPalpha

Incubation:

90 min at RT

Control Inhibitor:

hCGRPalpha

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

44308929

Name

hCGRPalpha

Measurement

0.058nM - IC50

PubChem ID

56841671

Name

Human adrenomedullin

Measurement

1.2nM - IC50

PubChem ID

118984394

Name

Calcitonin, human

Measurement

- IC50

PubChem ID

Name

MCP-4

Measurement

3nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

CGRP1 receptor agonism may cause or contribute to vasodilation, nociception, gastrointestinal mucous secretion, spasm and inflammation. CGRP1 receptor antagonism may have therapeutic as a spasmolytic, antidiarrheal, antiinflammatory and antinociception.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault