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。

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.

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.

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.

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

66990-30-5

C23H38O2

346.55

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years