PD 146176 Chemical Properties

Melting point:

160 °C

Boiling point:

485.4±24.0 °C(Predicted)

Density 

1.333±0.06 g/cm3(Predicted)

storage temp. 

Store at +4°C

solubility 

DMSO: 16 mg/mL, soluble

form 

solid

pka

16.17±0.20(Predicted)

color 

cream-colored

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

PD 146176 Usage And Synthesis

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.

Uses

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

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

PD 146176(4079-26-9)Related Product Information

• 15(S)-HPEDE
• CDC
• 5,8,11-EICOSATRIYNOIC ACID
• Caffeic acid
• BW B70C
• 15(S)-HEDE
• Esculetin
• REV 5901
• Baicalein
• PD 146176