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

PubChem ID

383414

Name

Octreotide

Measurement

0.0084μM - EC50

PubChem ID

5311430

Name

Seglitide

Measurement

0.013μM - EC50

PubChem ID

16133799

Name

BIM 23056

Measurement

0.13μM - EC50

PubChem ID

44291156

Name

Somatostatin-14

Measurement

0.000087μM - EC50

PubChem ID

70689318

Name

Vapreotide

Measurement

0.048μM - EC50

PubChem ID

Name

Cyclo-soamtostatin

Measurement

0.048μM - EC50

PubChem ID

Name

CYN 154806

Measurement

0.54μM - EC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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