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
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
HTRF
Testing Information
Incubation:
30 min at RT
Control Activator:
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 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
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
RELATED SOLUTIONS