PD-146176A potent and selective 15-LO inhibitor

PD-146176 (CAS 4079-26-9)

PD-146176 | CAS 4079-26-9 is rated 5.0 out of 5 by 1.
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Synonym: 6,11-Dihydro[1]benzothiopyrano[4,3-b]indole
Application: A potent and selective 15-LO inhibitor
CAS Number: 4079-26-9
Purity: ≥98%
Molecular Weight: 237.3
Molecular Formula: C15H11NS
* Refer to Certificate of Analysis for lot specific data (including water content).
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PD-146176 is a potent and selective inhibitor of 15-LO that suppresses oxidant stress-induced apoptosis in endothelial cells. Studies indicate that PD-146176 reduces atherosclerotic lesion development in New Zealand white rabbit through its nonspecific antioxidant properties. It is known that PD-146176 acts as a noncompetitive inhibitor towards 15-LO, displaying a Ki=197 nM. Furthermore, PD-146176 reduces monocyte macrophage enrichment of atherosclerotic lesions and development of fibrofoamy and fibrous plaque.


References

1. Sendobry, S.M., et al. 1997. Br. J. Pharmacol. 120: 1199-1206. PMID: 9105693
2. Bocan, T.M., et al. 1998. Atherosclerosis. 136: 203-216. PMID: 9543090
3. Kelavkar, U.P., et al. 2001. Carcinogenesis. 22: 1765-1773. PMID: 11698337
4. Sordillo, L.M., et al. 2005. Prostaglandins Other Lipid Mediat. 76: 19-34. PMID: 15967159
5. Succol, F. and Praticò, D. 2007. J. Neurochem. 103: 380-387. PMID: 17877641
6. Jeon, S.G., et al. 2009. Clin. Exp. Allergy. 39: 908-917. PMID: 19260872

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (50 mM), DMF&DMSO (~10 mg/ml), and 1:5 DMF:PBS (pH 7.2) (~0.15 mg/ml).
Storage :
Store at -20° C
Melting Point :
160.42° C (Predicted)
Boiling Point :
~485.45° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.77
IC50 :
15-LOX: IC50 = 0.54 µM (rabbit)
Ki Data :
15-LOX: Ki= 197 nM (rabbit)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
297589
MDL Number :
MFCD05664738
SMILES :
C1C2=C(C3=CC=CC=C3S1)NC4=CC=CC=C24

Download SDS (MSDS)

Certificate of Analysis

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PD-146176  Product Citations

See how others have used PD-146176. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 25301069  Skliris, A. et al. 2015. Cell Death Differ. 22: 703-18.

PMID: # 23559003  Xu, J. et al. 2013. Cell Death Dis. 4: e569.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Jeon et al Jeon et al. (PubMed ID 19260872) found that the 15-LO inhibitor, PD-146176, prevented dsRNA-induced allergic inflammation and recruitment of T cells following an allergen challenge in a Th1-allergic inflammation mouse model. -SCBT Publication Review
Date published: 2015-05-19
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