Biological Information

Background Information:

Angiotensin converting enzyme (ACE; kinase II, dipeptidyl carboxypeptidase), a zinc metalloprotease, is responsible for conversion of angiotensin I, generated by activation of the renin-angiotensin system, to angiotensin II; ACE also inactivates bradykinin and other potent vasodilators. Rapid metabolism of angiotensin I to angiotensin II in vivo is primarily due to activity of vascular tissue-bound ACE. Angiotensin II is clearly involved in malignant hypertension or hypertension resulting from stenosis of the renal artery as well as in some patients with normal plasma renin activity. Consequently, inhibitors of ACE are useful as antihypertensive agents; inhibition of bradykinin inactivation may produce dry cough.

Family:

Protease

Sub Family:

Angiotensin-Converting

Class:

Protein (enzyme)

Protein Name:

ACE

Uniprot Number:

P12821

Protein Aliases:

Dipeptidyl carboxypeptidase I

Gene Name:

ACE

Gene ID:

1636

Gene Aliases:

ACE1|CD143

Accession Number:

NM_000789

Organism:

Human

Construct Details:

Fragment (30-1261), Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Platform:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant angiotensin converting enzyme expressed in a mouse myeloma cell line is used. Test compound and/or vehicle is preincubated with 0.73 µg/ml of enzyme in modified MES buffer pH 6.5 for 15 minutes at 25°C. The reaction is initiated by addition of 25 µM Abz-FRK (Dnp)-P for another 30 minute incubation period. Determination of the amount of Abz-FR-OH formed is read spectrofluorimetrically at 320 nm/420 nm. Compounds are screened at 10 mM.

Substrate:

25 µM Abz-FRK (Dnp)-P

Incubation:

30 min at 25°C

Control Inhibitor:

Captopril

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

44093

Name

Captopril

Measurement

0.0054uM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP89
Item: PP223