4079-26-9 Usage
Description
PD 146176 is a potent and selective inhibitor of reticulocyte 15-lipoxygenase-1, a key enzyme involved in the metabolism of arachidonic acid. It has been shown to limit hypercholesterolemia-induced atherosclerosis in New Zealand White rabbits and reduce oxidant stress-induced apoptosis in endothelial cells. PD 146176 also inhibits amyloid β protein aggregate formation without changing total levels of amyloid β precursor protein (APP) in cells stably expressing APP. Furthermore, it lacks significant non-specific antioxidant properties.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 4079-26-9 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 4,0,7 and 9 respectively; the second part has 2 digits, 2 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 4079-26:
(6*4)+(5*0)+(4*7)+(3*9)+(2*2)+(1*6)=89
89 % 10 = 9
So 4079-26-9 is a valid CAS Registry Number.
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
4079-26-9Relevant articles and documents
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
Kang, Nana,Lee, Jung-Min,Jeon, Aeran,Oh, Han Bin,Moon, Bongjin
, p. 5612 - 5619 (2016)
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.
NOVEL TETRACYCLIC HETEROATOM CONTAINING DERIVATIVES USEFUL AS SEX STEROID HORMONE RECEPTOR MODULATORS
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Page/Page column 59-60, (2010/10/20)
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.
Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands
Zhang, Xuqing,Li, Xiaojie,Allan, George F.,Musto, Amy,Lundeen, Scott G.,Sui, Zhihua
, p. 3233 - 3237 (2007/10/03)
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