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- 文献和实验
- 技术资料
- CAS号:
131060-14-5
- 规格:
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥944.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥356.0 |
| 规格: | 5mg | 产品价格: | ¥856.0 |
| 规格: | 10mg | 产品价格: | ¥1456.0 |
| 规格: | 25mg | 产品价格: | ¥2920.0 |
| 规格: | 50mg | 产品价格: | ¥4144.0 |
| 规格: | 100mg | 产品价格: | ¥5704.0 |
Product Introduction
Bioactivity
| 名称 | NB-598 |
| 描述 | NB-598 is an effective and competitive inhibitor of squalene epoxidase. It suppresses triglyceride biosynthesis through the farnesol pathway. |
| 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 Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 140 mg/mL (311.34 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (22.24 mM), Solution. 10% DMSO+90% Corn Oil : 1 mg/mL (2.22 mM), Sonication is recommended. 10% DMSO+90% Saline : < 10 mg/mL (22.24 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. |
| 关键字 | Squalene epoxidase | NB-598 | NB598 | NB 598 | Inhibitor | inhibit |
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| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Fungal Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library | Anti-Cardiovascular Disease Compound Library | Neuronal Signaling Compound Library | Preclinical Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Covalent Inhibitor Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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