10,12-Tricosadiynoic acid 是一种高特异性，选择性，高亲和力且具有口服活性的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂。10,12-Tricosadiynoic acid 可改善线粒体脂质和 ROS 代谢，可用于高脂饮食或肥胖引起的代谢性疾病的研究。

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

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Acyl-CoA oxidase-1 (ACOX1).

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. 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 is the precursor of 10,12-Tricosadiynoic acid-CoA and is transformed into 10,12-Tricosadiynoic acid-CoA by peroxisomal very long chain acyl-CoA synthetase (VLACS) after entering into cells, and it inhibits ACOX1 in vivo.
10,12-Tricosadiynoic acid (500 nM) inhibits acyl-CoA oxidase-1 (ACOX1) activity. 10,12-Tricosadiynoic acid treatment

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 (adenosine 5′-monophosphate-activated protein kinase) 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.
10,12-Tricosadiynoic acid (0 mg/kg, 37.5 mg/kg, 75 mg/kg, and 150 mg/kg diet) treatment does not affect weight gain, but significantly decreases peroxisomal β-oxidation in the liver, and increased body fat accumulation in Nile tilapia. The fish with impaired peroxisomal β-oxidation exhibited higher contents of serum lipid and peroxidation products, and alanine aminotransferase act

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[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.
[2]. Takuto Chiba, et al. Sirtuin 5 Regulates Proximal Tubule Fatty Acid Oxidation to Protect against AKI. J Am Soc Nephrol. 2019 Dec;30(12):2384-2398.

In Vitro: DMSO : 100 mg/mL (288.56 mM; Need ultrasonic)配制储备液