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

PubChem ID

Name

Insulin

Measurement

0.19μM - IC50

PubChem ID

46861623

Name

Alvelestat

Measurement

>100μM - IC50

PubChem ID

107706

Name

Sivelestat

Measurement

4.1μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei