Biological Information
Background Information:
Pancreatic elastase 1, a serine proteinase, cleaves peptide bonds at the carbonyl end of amino acid residues with small hydrophobic side chains, such as glycine, valine, leucine, isoleucine, and particularly alanine. The wide specificity of elastase for non-aromatic uncharged side chains explains its unique ability to digest native elastin, a protein rich in aliphatic side chains. Pancreatic elastase 1 is also able to digest other proteins such as fibrin, hemoglobin, and casein, but not native collagen and keratin. Agents that inhibit pancreatic elastase may have clinical applications in treating chronic pancreatitis, cystic fibrosis, and pulmonary emphysema
Family:
Protease
Sub Family:
Chymotrypsin
Class:
Serine Peptidase
Protein Name:
Pancreatic Elastase 1
Uniprot Number:
P00772
Protein Aliases:
Elastase-1
Gene Name:
CELA1
Gene ID:
1990
Gene Aliases:
ELA1
Accession Number:
NM_001971
Organism:
Pig
Construct Details:
Endogenous
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Pig pancreas elastase is used. Test compound and/or vehicle is preincubated with 2.5 mU/ml enzyme in Tris-HCl buffer pH 8.0 for 15 minutes at 37˚C. The reaction is initiated by addition of 50 μM MeOSuc-Ala-Ala-Pro-Val-AFC for another 30-minute incubation period. Determination of the amount of AFC formed is read spectrofluorimetrically at Excitation: 380 nm; Emission: 500 nm. Compounds are screened at 10 μM.
Substrate:
50 μM MeOSuc-Ala-Ala-Pro-Val-AFC
Incubation:
30 min at 37°C
Control Inhibitor:
Sivelestat
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:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei