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:
DPP4
Uniprot Number:
P27487
Protein Aliases:
ADABP
Gene Name:
DPP4
Gene ID:
1803
Gene Aliases:
DPPIV
Accession Number:
NM_001935
Organism:
Human
Construct Details:
Fragment (29-766), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant DPP IV expressed in insect cells is used. Test compound and/or vehicle are preincubated with 42.5 ng/ml‡ of enzyme for 10 minutes at 25⁰C in Tris buffer pH 7.4. The reaction is initiated by addition of 40 µM GP-AMC for another 10 minute incubation period. Read plate on a spectrophotometer (Excitation: 355 nm, Emission: 460 nm). Compounds are screened at 10 μM.
Substrate:
40 µM GP-AMC
Incubation:
10 min at 25°C
Control Inhibitor:
UNII-74P4VV90RU
Criteria For Significance:
≥ 50 of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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