Biological Information

Background Information:

Renin (EC 3.4.23.15) is an aspartyl protease that is produced by the juxtaglomerular cells of the kidney. Renin catalyzes the conversion of angiotensinogen to angiotensin I. Angiotensin I is biologically inactive and is converted to angiotensin II by the angiotensin converting enzyme (ACE). Angiotensin II is a potent vasoconstrictor and increase the release of aldosterone. Active renin, angiotensin I, angiotensin II, and ACE are collectively known as the renin-angiotensin system (RAS).

Family:

Protease

Sub Family:

Pepsin

Class:

Aspartic Peptidase

Protein Name:

Renin

Uniprot Number:

P00797

Gene Name:

REN

Gene ID:

5972

Accession Number:

NM_000537

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 renin expressed in HEK cells is used. Test compound or vehicle with 0.2 μg/ml enzyme‡ is preincubated for 15 minutes at 37°C in modified HEPES buffer pH 7.4. The reaction is initiated by addition of 4 μM DABCYL-γ-Abu-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS for another 60 minutes incubation period. Determination of the amount of Val-Ile-His-Thr-EDANS formed is read spectrophotometrically at 325 nm/510 nm. Compounds are screened at 10 μM.

Substrate:

4 µM DABCYL-gamma-Abu-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS

Incubation:

60 min at 37°C

Control Inhibitor:

Cgp 29287

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

25078118

Name

Cgp 29287

Measurement

0.0042μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

The potent angiotensin II octapeptide liberated following renin and ACE action may contribute to hypertension, glomerular nephritis and cardiac hypertrophy.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei