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PD 146176

Cat. No. 2850

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Chemical Name: 6,11-Dihydro[1]benzothiopyrano[4,3-b]indole

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 (IC₅₀ = 0.54 μM for 15-LOX in rabbit reticulocytes). Lacks non-specific antioxidant properties and prevents atherogenesis via regulation of monocyte-macrophage enrichment in vivo.

Technical Data

M.Wt:

237.32

Formula:

C₁₅H₁₁NS

Solubility:

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Purity:

>98 %

Storage:

Store at +4°C

CAS No:

4079-26-9

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Sendobry et al (1997) Attenuation of diet-induced atherosclerosis in rabbits with a highly selective 15-lipoxygenase inhibitor lacking significant antioxidant properties. Br.J.Pharmacol. 120 1199. PMID: 9105693.

Bocan et al (1998) A specific 15-lipoxygenase inhibitor limits the progression and monocyte-macrophage enrichment of hypercholesterolemia-induced atherosclerosis in the rabbit. Atherosclerosis 136 203. PMID: 9543090.

Sordillo et al (2005) Enhanced 15-HPETE production during oxidant stress induces apoptosis of endothelial cells. Prostaglandins Other Lipid Mediat. 76 19. PMID: 15967159.

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