4079-26-9

Usage

Uses

Used in Pharmaceutical Research:
PD 146176 is used as a research tool for studying the role of 15-lipoxygenase-1 in various biological processes and diseases. Its ability to inhibit amyloid β protein aggregate formation makes it a valuable compound for investigating the underlying mechanisms of neurodegenerative disorders, such as Alzheimer's disease.
Used in Cardiovascular Research:
PD 146176 is used as a therapeutic agent for studying its potential in limiting hypercholesterolemia-induced atherosclerosis. Its ability to reduce oxidant stress-induced apoptosis in endothelial cells highlights its potential in the development of treatments for cardiovascular diseases.
Used in Inflammation and Immunology Research:
PD 146176 has been used to study its influence on ex vivo leukotriene B4 (LTB4) and lipoxin A4 (LXA4) secretion in adipose tissue. This research helps in understanding the role of 15-lipoxygenase-1 in inflammation and immune responses, which can be crucial for developing targeted therapies for inflammatory and autoimmune disorders.

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.

InChI:InChI=1/C15H11NS/c1-3-7-13-10(5-1)12-9-17-14-8-4-2-6-11(14)15(12)16-13/h1-8,16H,9H2

Upstream product

• 121113-04-0 1-thiochroman-4-one phenylhydrazone 
• 3528-17-4 2,3-dihydro-4H-[1]benzothiopyran-4-one 
• 100-63-0 phenylhydrazine 
• 7647-01-0 hydrogenchloride 
• 64-17-5 ethanol 
• 5219-65-8 acide phenylthio-3 propanoique 

Relevant academic research and scientific papers

Design and synthesis of new mass tags for matrix-free laser desorption ionization mass spectrometry (LDI-MS) based on 6,11-dihydrothiochromeno[4,3-b]indole

We have rationally designed and synthesized new mass tags that are heterolytically cleavable upon UV-irradiation; these tags are based on a 6,11-dihydrothiochromeno[4,3-b]indole skeleton. Unless exposed to UV light, the dithioacetal group maintained its stability under normal conditions. After chemical conjugation of the mass tags with biomolecules of interest, such as proteins, the resulting conjugates efficiently and selectively generated the corresponding mass-tag fragment ions without the aid of a matrix under laser desorption/ionization (LDI) conditions. We envision that these new dithioacetal-based tags would provide a new platform of the so-called matrix-free laser desorption ionization mass spectrometry (LDI-MS), that would allow multiple detection of biomarkers with high sensitivity and selectivity. The limit of detection (LOD) of these tags was measured to be 5?fmol in the case of non-conjugated mass tag themselves and 2.8?fmol in the case of mass-tag-conjugated myoglobin.

THIOCHROMENE TYPE COMPOUNDS AND THEIR USE

The present invention relates to a photodegradable mass tag material and a use thereof and, more specifically, to a thiochromene type compound and a use thereof. The thiochromene type compound can be helpfully used in matrix-assisted laser desorption/ionization time-of-flight mass spectrometry or matrix-less laser desorption/ionization time-of-flight mass spectrometry.

NOVEL TETRACYCLIC HETEROATOM CONTAINING DERIVATIVES USEFUL AS SEX STEROID HORMONE RECEPTOR MODULATORS

The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

NOVEL TETRACYCLIC HETEROATOM CONTAINING DERIVATIVES USEFUL AS SEX STEROID HORMONE RECEPTOR MODULATORS

The present invention is directed to novel tetracyclic heteroatom containing derivatives of formula (II), pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and proces

Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands

A novel series of tetracyclic indoles have been designed, synthesized and evaluated as androgen receptor (AR) ligands. Studies of structure-activity relationships (SARs) were investigated, which led to some compounds in this series as strong binders to an

Synthesis of Indole Derivatives

A one-step synthesis of indole derivatives in good yield through indolization of phenylhydrazones of cyclic keto compounds using formic acid is reported.