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
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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