Biological Information

Background Information:

There are three isoforms of NOS, each encoded by different genes: endothelial (eNOS), immune or inducible (iNOS) and neuronal (nNOS) nitric oxide synthase. They all form NO and L-citrulline by enzymatic oxidation of L-arginine. This reaction requires a number of cosubstrates, including molecular oxygen and tetrahydrobiopterin. Endothelial nitric oxide synthase (eNOS), which produces NO in physiological circumstances, plays an important role in regulation of vascular tone and reduction of atherosclerotic lesions. Inhibitors of eNOS may increase peripheral vascular resistance, platelet aggregation, cerebral and cardiac ischemia as well as decrease renal function and impair wound healing.

Family:

Nitrogen Metabolism

Sub Family:

Nitric Oxide Synthase

Class:

L-Arginine Turnover

Protein Name:

eNOS

Uniprot Number:

P29474

Protein Aliases:

endothelial nitric oxide synthase

Gene Name:

NOS3

Gene ID:

4846

Gene Aliases:

ECNOS|eNOS

Accession Number:

NM_000603

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Substrate:

[3H]arginine (28 nM) + arginine (50 nM)

Incubation:

30 min at 37°C

Control Inhibitor:

L-NMMA

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

2146

Name

Aminoguanidine

Measurement

- IC50

PubChem ID

6322

Name

L-arginine

Measurement

- IC50

PubChem ID

39836

Name

L-NAME

Measurement

- IC50

PubChem ID

135242

Name

L-NMMA

Measurement

300nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault