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PD146176

PD146176 (NSC-168807) 是一种 15-脂氧合酶(15-LO)抑制剂，抑制兔网织红细胞 15-LO，Ki 为 197 nM，IC50 为 0.54 μM。 它通过刺激老年三重转基因小鼠的自噬来逆转认知障碍、脑淀粉样变性和 tau 病理学。

CAS号

4079-26-9

分子式

C15H11NS

主要靶点

Autophagy|Lipoxygenase|Ferroptosis

仅限科研使用

Cat No : CM04974

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Synonyms

NSC168807

验证数据展示

  • CAS No.: 4079-26-9

    PD146176
    CAS#: 4079-26-9

产品信息

PD146176 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.

CAS号 4079-26-9
分子式 C15H11NS
主要靶点 Autophagy|Lipoxygenase|Ferroptosis
主要通路 自噬|代谢|凋亡
分子量 237.32
纯度 99.77%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 NSC168807

靶点活性

15-LO:IC50: 0.54 μM|15-LO:Ki: 197 nM

体外活性

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].

溶解度

DMSO:25 mg/mL (105.34 mM),Sonification is recommended.,H2O:< 0.1 mg/mL (insoluble)

参考文献

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.

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