PD 146176 is a potent and selective inhibitor of reticulocyte 15-lipoxygenase-1.1 It limits hypercholesterolemia-induced atherosclerosis in New Zealand White rabbits 2,1 and reduces oxidant stress-induced apoptosis in endothelial cells.3 PD 146176 inhibits amyloid β protein aggregate formation without changing total levels of amyloid β precursor protein (APP) in cells stably expressing APP.4 In addition, it lacks significant non-specific antioxidant properties.2
1
Bocan, T.M.A., Rosebury, W.S., Mueller, S.B., et al. A specific 15-lipoxygenase inhibitor limits the progression and monocyte-macrophage enrichment of hypercholesterolemia-induced atherosclerosis in the rabbit. Atherosclerosis136203-216(1998).
2
Sendobry, S.M., Cornicelli, J.A., Welch, K., et al. Attenuation of diet-induced atherosclerosis in rabbits with a highly selective 15-lipoxygenase inhibitor lacking significant antioxidant properties. Br J Pharmacol1201199-1206(1997).
3
Sordillo, L.M., Weaver, J.A., Cao, Y., et al. Enhanced 15-HPETE production during oxidant stress induces apoptosis of endothelial cells. Prostaglandins Other Lipid Mediat7619-34(2005).
4
Succol, F., and Praticò, D. A role for 12/15 lipoxygenase in the amyloid b precursor protein metabolism. J Neurochem103380-387(2007).
Synonyms
NSC 168807
Formal Name
6,11-dihydro-[1]benzothiopyrano[4,3-b]indole
CAS Number
4079-26-9
Molecular Formula
C15H11NS
Formula Weight
237.3
Formulation
A crystalline solid
Purity
≥98%
Stability
2 years
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
SMILES
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c1ccc2c(c1)SCc1c2[nH]c2ccccc12
Background Reading
Sendobry, S.M., Cornicelli, J.A., Welch, K., et al. Attenuation of diet-induced atherosclerosis in rabbits with a highly selective 15-lipoxygenase inhibitor lacking significant antioxidant properties. Br J Pharmacol1201199-1206(1997).
Bocan, T.M.A., Rosebury, W.S., Mueller, S.B., et al. A specific 15-lipoxygenase inhibitor limits the progression and monocyte-macrophage enrichment of hypercholesterolemia-induced atherosclerosis in the rabbit. Atherosclerosis136203-216(1998).
Succol, F., and Praticò, D. A role for 12/15 lipoxygenase in the amyloid b precursor protein metabolism. J Neurochem103380-387(2007).
Sordillo, L.M., Weaver, J.A., Cao, Y., et al. Enhanced 15-HPETE production during oxidant stress induces apoptosis of endothelial cells. Prostaglandins Other Lipid Mediat7619-34(2005).