Biological Information

Background Information:

Angiotensin-converting enzyme 2 (ACE2), identified human homolog of ACE, is a novel metalloprotease with specificity, tissue distribution (heart, lungs and kidneys), and function distinct from those of ACE. ACE2 may play a unique role in the renin-angiotensin system and mediate cardiovascular and renal function. Inhibitors of ACE2-specific peptide may be useful in the treatment of hypertension and other cardiovascular diseases.

Family:

Protease

Sub Family:

Angiotensin-Converting

Class:

Metallo Peptidase

Protein Name:

ACE2

Uniprot Number:

Q9BYF1

Protein Aliases:

peptidyl-dipeptidase A

Gene Name:

ACE2

Gene ID:

59272

Accession Number:

NM_001371415

Organism:

Human

Construct Details:

Fragment (18-740), 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 angiotensin converting enzyme-2 expressed in mouse myeloma cell line is used. Test compound and/or vehicle are preincubated with 45 ng/ml‡ of enzyme for 15 minutes at 25⁰C in Tris buffer pH 7.4. The reaction is initiated by addition of 10 µM of Mca-YVADAPK(Dnp)-OH for another 20 minute incubation period. Read plate on a spectrophotometer (Excitation: 340 nm, Emission: 430 nm). Compounds are screened at 10 μM.

Substrate:

10 μM Mca-Tyr-Val-Ala-Asp-Pro-Ala-Lys-(DNP)-OH

Incubation:

20 min at 25°C

Control Inhibitor:

Ac-GG-26-NH2

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

6049

Name

EDTA

Measurement

0.09μM - IC50

PubChem ID

44093

Name

Captopril

Measurement

>300μM - IC50

PubChem ID

Name

Ac-GG-26-NH2

Measurement

0.034μM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei