Neprilysin Inhibitor Screening Kit (Fluorometric), Human

Description

Neprilysin (NEP, EC 3.4.24.11), also known as neutral endopeptidase, enkephalinase, CD10 and common acute lymphoblastic leukemia antigen, is a type II zinc-containing transmembrane metalloproteinase. It can hydrolyze very important endogenous peptides, such as natriuretic atrial factor, enkephalin, substance P, bradykinin and amyloid β peptide. Therefore, NEP is a potential therapeutic target in important pathological conditions such as cardiovascular disease, prostate cancer, Alzheimer's disease and analgesics. NEP is also used as a biological marker for childhood leukemia called CALLA. NEP is currently the focus of cardiovascular and neurobiological research. NEP inhibitors have shown convincing results and can be used as a potential treatment alternative for certain diseases, including hypertension, heart failure, renal failure, and obesity in patients with type 2 diabetes. The combination of NEP inhibitor and type 1 angiotensin II receptor blocker has been used clinically to treat patients with chronic heart failure. Analysis Genie's NEP inhibitor screening kit can be used to screen potential inhibitors of NEP activity. It utilizes the ability of active NEP to cleave synthetic MCA-based peptide substrates to release free fluorophores. The released MCA can be easily quantified using a fluorescence microplate reader. In the presence of NEP specific inhibitors, the enzyme loses its activity, resulting in a decrease in fluorescence intensity. The assay kit is very simple and can be used to identify and characterize NEP inhibitors in a high-throughput format.

Species Reactivity

Human

Application Notes

Screening/characterizing/studying Neprilysin inhibitors/activators

Relevant Diseases

Neurological Disorders

Detection Method

Fluorometric (Ex/Em = 320/420 nm)

Assay Type

Inhibitor Screening Kit

Components

NEP Assay Buffer
NEP Enzyme (Lyophilized)
NEP Substrate (in DMSO) NEP Inhibitor (10 mM Thiorpan)

Shipping

Gel Pack

Storage

-20°C

Handling Advices

The antibody solution should be gently mixed before use.

Research Use Only

For research use only

Target

MME

Official Name

MME

Full Name

Membrane metallo-endopeptidase

Alternative Names

MME; Membrane metallo-endopeptidase

Gene ID

4311(Human); 17380(Mouse); 24590(Rat)

Uniprot ID

P08473(Human); Q61391(Mouse); P07861(Rat)

Figure 1 Inhibition of Neprilysin activity by Thiorphan. IC50 of Thiorphan was calculated to be 4.16 nM. Assay was carried out following the kit protocol.