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Novel Lipid Research Assay: Lysosomal PLA2 Inhibitor Screen

03-09-2017 02:48 PM CET | Health & Medicine

Press release from: MoBiTec GmbH

Lysosomal Phospholipase A2 (LPLA2) Inhibitor Scree

Lysosomal Phospholipase A2 (LPLA2) Inhibitor Scree

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 Echelon LPLA2 Inhibitor Screen (K-7000I) is a fluorogenic, high-throughput assay designed to identify problem compounds early in the drug discovery process leading to safer medicine.

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.

The Echelon LPLA2 Inhibitor Screen (K-7000I) 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.

Features:

· Novel Assay

· Consistent Results

· Easy-to-Use Format

· All Reagents Provided

· Sample Volume: 1 µl

· Sample Number: 128 Samples (in triplicates)/384-well plate

The Lysosomal PLA2 Inhibitor Screen is manufactured by Echelon Biosciences Incorporated (EBI), USA, and distributed in Europe by MoBiTec GmbH, Germany.

For product-specific details please see:

http://www.echelon-inc.com/index.php?module=Products&func=detail&id=958

Or contact us at info@mobitec.de

About MoBiTec GmbH

MoBiTec GmbH (Goettingen, Germany) is a privately held company (founded in 1987) that offers research tools for molecular and cell biology. Products include DNA vectors for cloning and expression, cell transfection reagents and cell culture tools, immobilized and soluble enzymes, products for genomics and proteomics research, numerous antibodies and recombinant proteins, superior fluorescence reagents and kits, affinity chromatography products, as well as general laboratory equipment.

In parallel to its own product lines, MoBiTec distributes products from international companies in Germany. MoBiTec products are distributed worldwide, in Germany from their home office, in other countries by distributors.

MoBiTec GmbH
Lotzestr. 22a
37083 Goettingen
Germany

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