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PD146176

Catalog No. T7530 CAS 4079-26-9

Synonyms: NSC168807

PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.

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PD146176, CAS 4079-26-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 41.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 275.00
100 mg	In stock	$ 482.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.77%

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Description	PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
Targets&IC50	15-LOX:IC50: 0.54 μM, 15-LOX:Ki: 197 nM
In vitro	15-LO by PD146176, an inhibitor of 15-LO with an IC50 in cells or isolated enzyme of 0.5-0.8 microM, may limit atherosclerotic lesion development through regulation of monocyte-macrophage enrichment.?Rabbits exposed to chronic endothelial denudation of the iliac-femoral artery were meal-fed a 0.25% cholesterol (C), 3% peanut oil (PNO), 3% coconut oil (CNO) diet twice daily with and without 175 mg/kg PD146176 for 12 weeks.?In a second study, atherosclerotic lesions were pre-established in rabbits through chronic endothelial denudation and meal-fed a 0.5% C, 3% PNO, 3% CNO diet for 9 weeks and a 0% C/fat diet for 6 weeks prior to an 8 week administration of PD146176 at 175 mg/kg,?q.d. Plasma total and lipoprotein cholesterol exposure were similar in control and PD146176-treated animals in both studies but PD146176 increased plasma triglyceride exposure 2- to 4-fold.?Plasma PD146176 concentrations ranged from 99 to 214 ng/ml at 2 h post-dose.?In the progression study, the iliac-femoral monocyte-macrophage area was reduced 71%, cross-sectional lesion area was unchanged and cholesteryl ester (CE) content was reduced 63%.?In the regression study, size and macrophage content of iliac-femoral, fibrous plaque-like lesions were decreased 34%, CE content was reduced 19% and gross extent of thoracic aortic lesions were reduced 41%.?PD146176 can limit monocyte macrophage enrichment of atherosclerotic lesions and can attenuate development of fibrofoamy and fibrous plaque lesions in the absence of changes in plasma total or lipoprotein cholesterol concentrations[1].

Synonyms	NSC168807
Molecular Weight	237.32
Formula	C15H11NS
CAS No.	4079-26-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (105.34 mM), Sonification is recommended.

H2O: < 0.1 mg/mL (insoluble)

References and Literature

1. Bocan TM, et al. A specific 15-lipoxygenase inhibitor limits the progression and monocyte-macrophage enrichment of hypercholesterolemia-induced atherosclerosis in the rabbit [published correction appears in Atherosclerosis 1998 Jul;139(1):201]. Atherosclerosis. 1998;136(2):203-216. 2. Sendobry SM, et al. Attenuation of diet-induced atherosclerosis in rabbits with a highly selective 15-lipoxygenase inhibitor lacking significant antioxidant properties. Br J Pharmacol. 1997;120(7):1199-1206. 3. Di Meco A, et al. 12/15-Lipoxygenase Inhibition Reverses Cognitive Impairment, Brain Amyloidosis, and Tau Pathology by Stimulating Autophagy in Aged Triple Transgenic Mice. Biol Psychiatry. 2017;81(2):92-100.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Metabolism Compound Library Bioactive Compound Library NO PAINS Compound Library Autophagy Compound Library Bioactive Compounds Library Max Ferroptosis Compound Library Cell Cycle Compound Library Apoptosis Compound Library

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Keywords

PD146176 4079-26-9 Apoptosis Autophagy Metabolism Ferroptosis Lipoxygenase inhibit tau PD 146176 brain triple NSC-168807 pathology amyloidosis transgenic reticulocyte impairment NSC168807 cognitive mice PD-146176 Inhibitor cells IC21 rabbit NSC 168807 inhibitor

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