PD 146176

Description

PD 146176 is a potent and selective inhibitor of reticulocyte 15-lipoxygenase-1. It limits hypercholesterolemia-induced atherosclerosis in New Zealand White rabbits and reduces oxidant stress-induced apoptosis in endothelial cells. PD 146176 inhibits amyloid β protein aggregate formation without changing total levels of amyloid β precursor protein (APP) in cells stably expressing APP. In addition, it lacks significant non-specific antioxidant properties.

The Uses of PD 146176

PD 146176 has been used to study its influence on ex vivo leukotriene B4 (LTB4) and lipoxin A4 (LXA4) secretion in adipose tissue.

What are the applications of Application

PD-146176 is a potent and selective 15-LO inhibitor

Definition

ChEBI: PD-146176 is an organic heterotetracyclic compound that is 1H-indole which is ortho-fused to a 2H-1-benzothiopyran group at positions 2-3. It is an inhibitor of 15-lipoxygenase that limits atherosclerotic lesion development in rabbits. It has a role as a ferroptosis inhibitor, an EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor and an antiatherogenic agent. It is an organic heterotetracyclic compound, an organosulfur heterocyclic compound and an organonitrogen heterocyclic compound.

Biological Activity

Specific, non-competitve 15-lipoxygenase (15-LOX) inhibitor (K i = 197nM) that has no demonstrable effect on 5-LOX, 12-LOX, COX-1 or COX-2 (IC 50 = 0.54 μ M for 15-LOX in rabbit reticulocytes). Lacks non-specific antioxidant properties and prevents atherogenesis via regulation of monocyte-macrophage enrichment in vivo .

Biochem/physiol Actions

PD 146176 blocks neuroprotectin D1 (NPD1) and eicosanoid synthesis by inhibiting the 5-lipoxygenase-1 (15-LOX-1) enzyme.

Storage

Store at +4°C