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- 技术资料
- CAS号：
1698878-14-6
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥697.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥265.0 |
| 规格： | 2mg | 产品价格： | ￥362.0 |
| 规格： | 5mg | 产品价格： | ￥630.0 |
| 规格： | 10mg | 产品价格： | ￥1112.0 |
| 规格： | 25mg | 产品价格： | ￥2184.0 |
| 规格： | 50mg | 产品价格： | ￥3304.0 |
| 规格： | 100mg | 产品价格： | ￥4712.0 |
Product Introduction
Bioactivity
| 名称 | Nampt-IN-1 |
| 描述 | Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM. |
| 细胞实验 | The cell lines used as following: A2780 and KM-12, KMS-11 and MKN-74, OPM-2 and Kelly; and all other cancer cells. Cells are seeded in 96-well plates, cultured overnight, and treated with LSN3154567 (0.03 to 1,000 nM)±NA (10 μM) in duplicate at 37°C in 5% CO2 for 72 hours. Staurosporine (10 μM) is used as positive control. Cell viability is determined by a CytoTox-Glo Cytotoxicity assay kit. |
| 动物实验 | Male CD-1 mice are dosed with LSN3154567 at 2 mg/kg intravenously in 20% Captisol (w/v), 25 mmol/L NaPO4, pH 2, q.s. formulation or 2 mg/kg orally in the same vehicle in a cross over design with 3-d wash period in between two arms. Blood samples are obtained through retro orbital at 0, 0.08 (IV only), 0.25, 0.75, 2, 4, 8, and 24 hours and frozen until analysis. For exposure analysis, blood samples (≈20 μL) are obtained through tail clipping at 0.5, 1, 2, 4, 8, and 24 hours. The samples are collected into EDTA-coated capillary tubes and spotted onto Whatman DMPK-C DBS collection cards. |
| 体外活性 | LSN3154567 inhibits purified NAMPT with an IC50 of 3.1 nM. When tested against a panel of human kinases (>100; CEREP Kinase panel), it does not exhibit any significant activity (i.e.: IC50≥1 μM) against the kinases tested except CSF1R (IC50≈0.84 μM). To assess its anticancer activity, LSN3154567 is tested against a number of different types of cancer cell lines cultured in the absence or presence of nicotinic acid (NA) (10 μM). LSN3154567 exhibits a potent antiproliferative activity against many cell lines in the absence of NA. |
| 体内活性 | When dosed orally with 2 mg/kg in mice, it has an exposure of 195 nM*hour in the plasma with a peak concentration of 57 nM (at 0.25 hour) and an oral bioavailability of 39%. When dosed intravenously with 2 mg/kg, it has a hepatic clearance of 158.73 mL/min/kg and a volume of distribution at 7.1 L/kg. The half-life of terminal elimination is estimated to be 2.76 hours. LSN3154567 exhibits a dose-dependent inhibition of NAD+ formation with estimated TED50 value of 2.0 mg/kg. Dogs are treated with LSN3154567 at 1 and 2.5 mg/kg. At these dose levels, the retinal toxicity is observed. Degeneration of the outer nuclear layer occurred in all four animals, but is less pronounced in the animals treated with 1 mg/kg. |
| 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 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.77 mM), Sonication is recommended. DMSO : 55 mg/mL (131.11 mM), Sonication is recommended. |
| 关键字 | Visfatin | Pre-B cell colony enhancing factor | PBEF | Nicotinamide phosphoribosyl transferase | Nampt-IN-1 | NamptIN1 | Nampt IN 1 | NAMPT | LSN-3154567 | LSN 3154567 | Inhibitor | inhibit | CSF-1R | CSF1R | cFms |
| 相关产品 | Onatasertib | Cerdulatinib hydrochloride | GW786034B | Sotuletinib | PLX647 | GW2580 | Tandutinib | Dovitinib | c-Fms-IN-13 | Pexidartinib | PLX5622 | Nampt activator-1 |
| 相关库 | Inhibitor Library | Immuno-Oncology Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Cytokine Inhibitor Library | Metabolism Compound Library | Kinase Inhibitor Library | NO PAINS Compound Library | Glycometabolism Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Metabolism Disease Compound Library |
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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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化合物 Nampt-IN-1【1698878-14-6】
￥265 - 4712
