Biological Information

Background Information:

Tryptase is the predominant protein in mast cell granules. Tryptase activates protease activated receptors (PARs)-PAR-1, -3, -4, pro-thrombin, pro-MMP-3, Pro-MMP-1, pro-TGF-b, complement C3, prekallikrein and pro-urokinase plasminogen activator. Allergic or inflammatory stimulation activates mast cells triggering tryptase release. Inhibitors of tryptase have clinical benefits for mast cell-mediated diseases such as asthma.

Family:

Protease

Sub Family:

Chymotrypsin

Class:

Serine Peptidase

Protein Name:

Tryptase

Uniprot Number:

Q15661.1

Protein Aliases:

Tryptase I;Tryptase alpha-1

Gene Name:

TPSAB1

Gene ID:

7177

Gene Aliases:

tryptase alpha II;tryptase beta I;tryptase-I;tryptase-II;tryptase-III;mast cell tryptase

Accession Number:

NM_003294

Organism:

Human

Construct Details:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Matured human recombinant tryptase expressed in mouse myeloma cell line is used. Test compound and/or vehicle is preincubated with 104 ng/ml enzyme in modified Tris-HCl buffer pH 8.5 for 15 minutes at 25˚C. The reaction is initiated by addition of 30 μM Z-Gly-Pro-Arg-AMC for another 30-minute incubation period. Determination of the amount of AMC formed is read spectrofluorimetrically at 360 nm/465 nm. Compounds are screened at 10 μM.

Substrate:

30 µM Z-Gly-Pro-Arg-AMC

Incubation:

30 min at 25°C

Control Inhibitor:

CRA-2059

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

119

Name

4-aminobutyric acid

Measurement

0.00012μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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