Biological Information

Background Information:

Dipeptidyl peptidase 4 (DPP4; DPP IV, CD26) is a serine exopeptidase that cleaves X-proline dipeptides from the N terminus of polypeptides. It is an intrinsic membrane glycoprotein anchored into the cell membrane by its N-terminal end. High levels of the enzyme are found in the brush-border membranes of the kidney proximal tubule and of the small intestine, but several other tissues also express the enzyme. It has been suggested that physiological concentrations of GLP-1 (glucagon-like peptide-1) are degraded by DPP IV and the inhibitors of DPP IV may be a useful adjunct in the management of type II diabetes. Inhibitors of DPP IV may also be useful in reducing immune responses (asthma) as well as inflammation.

Family:

Protease

Sub Family:

Prolyl Oligopeptidase

Class:

Serine Peptidase

Protein Name:

Dipeptidyl Peptidase 4

Uniprot Number:

P27487

Gene Name:

DPP4

Gene ID:

1803

Gene Aliases:

DPPIV

Accession Number:

NM_001935

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Substrate:

GP-AMC, fluorogenic substrate (40 µM)

Incubation:

10 min at RT

Control Inhibitor:

UNII-74P4VV90RU

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

9818824

Name

UNII-74P4VV90RU

Measurement

3.7nM - IC50

PubChem ID

71433965

Name

P32/98

Measurement

120nM - IC50

PubChem ID

11522448

Name

Talabostat

Measurement

0.306nM - IC50

PubChem ID

49800073

Name

Saxagliptin

Measurement

1.35nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault