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10,12-Tricosadiynoic acid

10,12-Tricosadiynoic acid 是一种口服有效的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂，具有高特异性，选择性，高亲和力的特点。10,12-Tricosadiynoic acid 可改善线粒体脂质和 ROS 代谢，在高脂饮食或肥胖引起的代谢性疾病中有研究的价值。

CAS号

66990-30-5

分子式

C23H38O2

主要靶点

Acyltransferase

仅限科研使用

Cat No : CM20704

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Synonyms

TCDA|TDA

验证数据展示

  • CAS No.: 66990-30-5

    10,12-Tricosadiynoic acid
    CAS#: 66990-30-5

产品信息

10,12-Tricosadiynoic acid is a highly selective and orally active inhibitor of acyl-CoA oxidase-1 (ACOX1). It can treat the high-fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism.

CAS号 66990-30-5
分子式 C23H38O2
主要靶点 Acyltransferase
主要通路 代谢
分子量 346.55
纯度 ， 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 TCDA|TDA

体内活性

10,12-Tricosadiynoic acid (100 μg/kg; oral gavage; daily; for 8 weeks; male Wistar rats) treatment increases hepatic mitochondrial fatty acid oxidation (FAO) via activation of the SIRT1-AMPK pathway and proliferator activator receptor α and reduces hydrogen peroxide accumulation in high fat diet-fed rats, which significantly decreases hepatic lipid and ROS contents, reduces body weight gain, and decreases serum triglyceride and insulin levels.

体外活性

10,12-Tricosadiynoic acid-CoA rapidly inhibits ACOX1 activity in a time- and concentration-dependent manner. The activity of ACOX1 decreases by nearly 95% after 5 min of incubation with 10 eq of 10,12-Tricosadiynoic acid-CoA. ACOX1 activity is inhibited only if free 10,12-Tricosadiynoic Acid is activated as the CoA thioester, the substrate form. The inhibition of ACOX1 by 10,12-Tricosadiynoic acid-CoA is irreversible. And the kinetics parameters KI and kinact are calculated to be 680 nm and 3.18/min, respectively.

溶解度

DMSO:2.75 mg/mL (7.94 mM)

动物实验

Animal Model: Male Wistar rats (210-230 g) fed with high-fat diet. Dosage: 100 μg/kg. Administration: Oral gavage; daily; for 8 weeks

参考文献

1.Zeng J, et al. Specific Inhibition of Acyl-CoA Oxidase-1 by an Acetylenic Acid Improves Hepatic Lipid and Reactive Oxygen Species (ROS) Metabolism in Rats Fed a High Fat Diet. J Biol Chem. 2017 Mar 3;292(9):3800-3809.

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