Biological Information

Background Information:

5-Lipoxygenase catalyzes the oxidative metabolism of arachidonic acid to 5-hydroxyeicosatetraenoic acid (5-HETE), the initial reaction leading to formation of leukotrienes. Leukotrienes (LTs) are inflammatory mediators causing, for example, phagocyte chemotaxis and increased vascular permeability. Inhibition of LT biosynthesis may be beneficial in inflammatory diseases.

Family:

Lipid Metabolism

Sub Family:

Eicosanoid Turnover

Class:

Lipoxygenase

Protein Name:

5-LO

Uniprot Number:

P09917

Protein Aliases:

Arachidonate 5-lipoxygenase B, 5-LO

Gene Name:

ALOX5

Gene ID:

240

Gene Aliases:

5-LOX

Accession Number:

NM_000698

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:

Human recombinant 5-LO expressed in insect Sf9 cells is used. Test compound or vehicle are preincubated with 1.4 U/mlǂ of enzyme for 15 minutes at 25°C in Tris buffer pH 7.4. The reaction is initiated by addition of 10 µM arachidonyl amide and dye DHR123 for another 20 minute incubation period. Read plate on a spectrophotometer (Excitation: 485 nm, Emission: 535 nm). Compounds are screened at 10 µM.

Substrate:

10 µM AMC Arachidonoyl Amide

Incubation:

20 min at 25°C

Control Inhibitor:

NDGA

Criteria For Significance:

≥ 50 of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

57654453

Name

Nordihydroguaiaretic acid

Measurement

0.43µM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei