Icosabutate 是一种具有口服活性的 ω-3多不饱和脂肪酸，是二十碳五烯酸的衍生物 (EPA derivative)。Icosabutate 克服了未经修饰的 EPA 对肝脏靶向的缺点，可改善了胰岛素敏感性，肝炎和纤维化。Icosabutate 具有良好的耐受性，可有效降低持续性高甘油三酯血症中的非高密度脂蛋白胆固醇 (non-HDL-C) 水平。

Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia .

Liquid

IC50: non-HDL-C

Icosabutate (oral gavage; 100 mg/kg; once) accounts for the much higher flow rate of portal vein plasma (522 mL/h) versus mesenteric lymph (0.5 mL/h), that data demonstate that icosabutate is almost entirely taken up through the portal vein (>99%) with only a small fraction of icosabutate being absorbed through the lymphatic pathway in 8‐week old male Wistar rats.
Icosabutate ([14‐C]‐icosabutate; oral gavage; 100 mg/kg; once) shows that peak concentrations of radioactivity in most tissues at 4‐8 hours after the dose (except the gastrointestinal tract) with highest concentrations in the liver and kidney, most other tissues contain levels of radioactivity below that in plasma in male albino Wistar rats.
Icosabutate (diet administration; 135 mg/kg/day; 5 weeks) markedly improved glucose tolerance after an oral glucose load, significantly reduces AU

Room temperature in continental US; may vary elsewhere.

Pure form -20°C 3 years；In solvent -80°C 6 months

[1]. van den Hoek AM, et al. Icosabutate Exerts Beneficial Effects Upon Insulin Sensitivity, Hepatic Inflammation, Lipotoxicity, and Fibrosis in Mice.Hepatol Commun. 2019 Dec 24;4(2):193-207.
[2]. Kastelein JJ, et al. Icosabutate, a Structurally Engineered Fatty Acid, Improves the Cardiovascular Risk Profile in Statin-Treated Patients with Residual Hypertriglyceridemia.Cardiology. 2016;135(1):3-12.

In Vitro: DMSO : 100 mg/mL (266.98 mM; Need ultrasonic)配制储备液