muscle fatty acid oxidation

CP-640186 是一种有效的乙酰辅酶 A 羧化酶 (ACC)抑制剂，抑制大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50分别为 53 nM 和 61 nM。

CP-640186 hydrochloride (CP 640186 HCl) 是膜渗透性的乙酰辅酶A 羧化酶（ACC）抑制剂，抑制大鼠肝脏ACC1和大鼠骨骼肌ACC2的IC50为53 nM 和61 nM。

P053 是一种有效的，非竞争性和选择性的神经酰胺合酶1 (CerS1) 抑制剂（IC50= 0.5 μM）。P053 作为肌肉线粒体脂肪酸氧化的内源性抑制剂和全身肥胖调节剂。

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

(±)17-HDHA is an autoxidation product of docosahexaenoic acid in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. 17(S)-HDHA could be produced by enzymatic oxidation of DHA using soybean lipoxygenase (LO) and is the putative product of mammalian 15-LOs. 17(S)-HDHA was shown to be an inhibitor of U-46619 -induced rabbit and rat aortic smooth muscle contraction with IC50 values of 4.9 and 7.2 μM, respectively. (±)17-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.

CPT2 (Carnitine palmitoyltransferase 2) 是一种脂肪酸氧化过程中的酶，它在结直肠癌 (CRC) 预后评估中作为生物标志物。CPT2 通过过表达激活p-p53并增加p53蛋白水平，这有助于抑制肿瘤生长和促进细胞的凋亡。CPT2 缺乏是长链脂肪酸氧化障碍相关的常见遗传性疾病，并且CPT2 的表达降低与多种癌症的发展密切相关，因此，在癌症研究领域具有研究价值。