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 tissue and within the central nervous sytem. Agonism at SRIF1B (sst5) receptors may inhibit release of growth hormone (GH) and insulin from pituitary and pancreas and reduce vascular smooth muscle cell proliferation.

Family:

GPCR

Sub Family:

Somatostatin

Class:

Class A

Protein Name:

sst5

Uniprot Number:

P35346

Protein Aliases:

SS5-R|SS5R

Gene Name:

SSTR5

Gene ID:

6755

Accession Number:

NM_001053

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]Tyr11-somatostatin-14

Ligand Kd (nM):

0.2

Ligand Concentration:

0.1 nM

Non Specific:

1 µM Somatostatin-14

Incubation:

120 min at RT

Control Inhibitor:

Somatostatin-14

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:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

16133799

Name

BIM 23056

Measurement

17nM - IC50

PubChem ID

16133849

Name

Somatostatin 1-28

Measurement

0.3nM - IC50

PubChem ID

44291156

Name

Somatostatin-14

Measurement

0.4nM -

PubChem ID

Name

[D-Trp8]somatostatin

Measurement

0.25nM - Ic50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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