Biological Information

Background Information:

Phospholipase A2 (PLA2) is a key limiting step in the release of arachidonic acid (AA) by breaking down phospholipids for eicosanoid generation to form several inflammatory and thrombogenic molecules. PLA2 are usually categorized into four broad families, 15 group types in biochemical characteristics. Each of these types has been implicated in diverse kinds of lipid metabolism and disease progress. The group V sPLA2 (secretory phospholipase A2) has been implicated in AA release in major immunoinflammatory such as macrophages and mast cells cells. Excess level of sPLA2 is thought to contribute to promote vascular inflammation correlating with coronary events in coronary artery disease and coronary syndrome. Identification of selective sPLA2 inhibitors may offer substantial aid in treatment of the various pathological situations including atherosclerosis.

Family:

Lipid Metabolism

Sub Family:

Glycerophospholipid Turnover

Class:

Phospholipase A2

Organism:

Human

Construct Details:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrophotometry

Measured Response:

Absorbance

Testing Information

Procedure Summary:

Human recombinant sPLA2-V expressed in E. coli cells is used. Test compound or vehicle and DTNB are preincubated with 1 µg/ml‡ of enzyme for 15 minutes at 25⁰C in Tris buffer. The reaction is initiated by addition of 0.25 mM Diheptanoyl Thio-PC for another 30 minute incubation period. Read plate on a spectrophotometer at 405 nm. Compounds are screened at 10 μM.

Substrate:

250 µM diheptanoyl thio-PC

Incubation:

30 min at 25°C

Control Inhibitor:

LY311727

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

155922

Name

LY311727

Measurement

3.9μM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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