化合物NB-598 TQ0115

Product Introduction
Bioactivity


英文名: NB-598

描述: NB-598 是一种鲨烯环氧化酶竞争性抑制剂，可以阻碍甘油三酯的生物合成。

激酶实验: Caco-2 cells are grown in a 58 cm2 plastic dish with medium A for 13 days. The cells are washed with medium B, and then cultured with medium B including cholesterol-micelle and each compound. The compound is dissolved in Me2SO, and the final concentration of Me2SO is 0.1%(v/v). After 18 hr of incubation, the cells are washed extensively with phosphate-buffered saline (PBS) to remove the compound. Microsomes are prepared as described above. The reaction mixture (0.2 mL) consisted of 0.1 mg microsomes, 0.25% BSA and 40 PM [14C]oleoyl CoA in buffer A. To avoid the effects of endogenous cholesterol, liposome (2 mol of cholesterol: 1 mol of phosphatidylcholine) [15] is added to the reaction mixture. The microsomes are preincubated for 1 hr with or without exogenous cholesterol, and ACAT activity is determined as described above [1].

体外活性: NB-598（10 μM）能够抑制来自[14C]乙酸的固醇和固醇酯的合成，而不影响其他脂质如磷脂（PL）、游离脂肪酸（FFA）和三酰甘油（TG）的合成。在无外源性脂质体胆固醇的条件下，NB-598降低ACAT活性31%。即使在含600 pM脂质体胆固醇的环境中，NB-598也能降低ACAT活性22%[1]。NB598（10 μM）导致MIN6细胞总胆固醇水平降低36±7%。NB598显著降低PM、ER和SG处的胆固醇，分别下降49±2%、46±7%和48±2%。NB598剂量依赖性地抑制胰岛素分泌，在基础（1 mM葡萄糖）和葡萄糖刺激（16.7 mM葡萄糖）条件下均是如此。NB598在高达10 μM的浓度下，不影响KV电流的峰值外向电流或激活的电压依赖性，但会增加电流的失活[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mg/mL (22.24 mM)


关键字: inhibit | Inhibitor | NB598 | NB 598 | NB-598

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