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PD146176

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

cognitive|cells|Autophagy|brain|15-LO|amyloidosis|Ferroptosis|inhibit|impairment|IC21|NSC 168807|NSC168807|NSC-168807|PD146176|PD-146176|PD 146176|pathology|reticulocyte|rabbit|Inhibitor|mice|tau|triple|transgenic

验证数据展示

  • CAS No.: 4079-26-9

    PD146176
    CAS#: 4079-26-9

产品信息

CAS号 4079-26-9
分子式 C15H11NS
主要靶点 Autophagy|Lipoxygenase|Ferroptosis
主要通路 凋亡|代谢|自噬
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 | Shipping with blue ice.
别名 cognitive|cells|Autophagy|brain|15-LO|amyloidosis|Ferroptosis|inhibit|impairment|IC21|NSC 168807|NSC168807|NSC-168807|PD146176|PD-146176|PD 146176|pathology|reticulocyte|rabbit|Inhibitor|mice|tau|triple|transgenic

靶点活性

15-LOX:IC50: 0.54 μM|15-LOX:Ki: 197 nM

体外活性

15-LO通过PD146176（一种IC50在细胞或单独酶中为0.5-0.8 microM的15-LO抑制剂）可能通过调节单核细胞-巨噬细胞的富集来限制动脉粥样硬化斑块的发展。在慢性内皮剥脱的股髂动脉的兔子上进行的实验中，给予0.25%胆固醇（C）、3%花生油（PNO）、3%椰子油（CNO）的饮食，每日两次，连同175 mg/kg PD146176共持续12周。在第二项研究中，通过慢性内皮剥脱在兔子上预先建立动脉粥样硬化斑块，之后给予0.5% C、3% PNO、3% CNO饮食9周和0% C/脂肪饮食6周，然后连续8周每天给予175 mg/kg PD146176。在两项研究中，对照组和PD146176处理组的动物的血浆总胆固醇和脂蛋白胆固醇暴露程度相似，但PD146176使血浆甘油三酯暴露量增加了2至4倍。血浆PD146176浓度在剂量后2小时范围为99至214 ng/ml。在进展研究中，股髂动脉单核细胞-巨噬细胞区域减少了71%，横截面斑块区域未变，而胆固醇酯（CE）含量减少了63%。在回归研究中，股髂动脉纤维斑块样病变的大小和巨噬细胞含量减少了34%，CE含量减少了19%，胸主动脉病变的总体程度减少了41%。PD146176能够限制动脉粥样硬化斑块中的单核细胞巨噬细胞的富集，并且在血浆总胆固醇或脂蛋白胆固醇浓度未改变的情况下，减缓纤维泡沫状和纤维斑块病变的发展。

溶解度

DMSO:25 mg/mL (105.34 mM);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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