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
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