Innovative Tools for Molecular and Cell Biology

Innovative Tools for Molecular and Cell Biology

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Exclusive Inhibitor Screen for Phospholipidosis (PL)

Lysosomal PLA2 Inhibitor Screen

LPLA2-Inhibitor-Screen

Lysosomal PLA2 Inhibitor Screen

Features

  • Novel lipid research assay
  • Consistent results
  • Easy-to-use format
  • All reagents provided

Description

  • Inhibition of Lysosomal Phospholipase A2 (LPLA2) by a drug candidate can predict its potential to cause drug-induced phospholipidosis, a serious side effect resulting in tissue inflammation and organ damage.
  • The LPLA2 Inhibitor Screen is a fluorogenic, high throughput assay designed to identify problematic compounds early in the drug discovery process leading to safer medicines.

Application

  • Human lysosomal phospholipase A2 (LPLA2) is responsible for normal lipid metabolism and it is unique from other known PLA2s in that LPLA2 is only active in an acidic environment (~pH 4.5). Phospholipidosis (PL) is a condition resulting from the excessive accumulation of intracellular phospholipids, causing tissue inflammation and organ damage. PL can manifest in patients taking certain cationic amphiphilic drugs (CADs) such as Fluoxetine (Prozac™, Sarafem) and Amiodarone. The FDA has determined that drug-induced phospholipidosis (DIPL) is a serious drug safety issue and evidence is accumulating that DIPL is the result of certain CADs directly inhibiting LPLA2.

  • Echelon’s LPLA2 Inhibitor Screen is designed to assay a drugs ability to inhibit LPLA2 activity in vitro, and thus potentially predict drug-induced phospholipidosis. The assay uses a quenched substrate which fluoresces when hydrolyzed by LPLA2. This direct biochemical approach provides a quantitative measurement in a robust and simple-to-use in vitro plate-based assay, providing greatly increased throughput when compared to traditional microscopy methods of tissue cultured cells. The assay has been validated with a group of known PL-inducing and non-PL inducing drugs. The known PL-inducing cationic amphiphilic drug, Amiodarone, is included in the assay as a control.

ORDER INFORMATION

  • For shipping and storage information please click on Order#.
Order# Description Amount Price Data Sheet
K-7000I-EC Lysosomal Phospholipase A2 (LPLA2) Inhibitor Screen 1 ea 678,00 PDF
  • All prices are in EURO excl. VAT and shipping. Only available in Europe except for France and Italy.