Biological Information
Background Information:
Somatostatin (somatotropin-release inhibiting factor, SRIF) receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. The five known receptors can be divided into two groups: SRIF1 (SRIF1A=sst2, SRIF1B=sst5, srif1C=sst3) and SRIF2 (SRIF2A=sst1, srif2B=sst4); lower case (srif) indicates an as yet undefined physiological role. SRIF receptors are found in most peripheral tissues and within the central nervous sytem.
Family:
GPCR
Sub Family:
Somatostatin
Class:
Class A
Protein Name:
sst3
Uniprot Number:
P32745
Protein Aliases:
SS3-R|SS3R|SSR-28
Gene Name:
SSTR3
Gene ID:
6753
Accession Number:
XM_011530349
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant somatostatin sst3 receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (2 x 10^5 /ml) in incubation buffer for 20 minutes at 37°C. Test compound-induced decrease of cAMP by 50 percent or more (≥50%) relative to the 1 μM somatostatin-14 response indicates possible sst3 receptor agonist activity.
Incubation:
20 min at 37°C
Control Activator:
Somatostatin-14
Criteria For Significance:
≥ 50% decrease in cAMP relative to Somatostatin-14 response, ≥ 50% Inhibition of Somatostatin-induced cAMP decrease
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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