Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nampt-IN-1 (LSN3154567) 是选择性的 NAMPT 抑制剂,能够抑制纯化的 NAMPT,IC50=3.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 312 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,730 | 现货 | ||
50 mg | ¥ 4,130 | 现货 | ||
100 mg | ¥ 5,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 872 | 现货 |
产品描述 | 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. |
靶点活性 | CSF1R:0.84 μM, NAMPT:3.1 nM |
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. |
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. |
别名 | LSN3154567 |
分子量 | 419.49 |
分子式 | C20H25N3O5S |
CAS No. | 1698878-14-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (131.11 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3838 mL | 11.9192 mL | 23.8385 mL | 59.5962 mL |
5 mM | 0.4768 mL | 2.3838 mL | 4.7677 mL | 11.9192 mL | |
10 mM | 0.2384 mL | 1.1919 mL | 2.3838 mL | 5.9596 mL | |
20 mM | 0.1192 mL | 0.596 mL | 1.1919 mL | 2.9798 mL | |
50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1919 mL | |
100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.596 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Nampt-IN-1 1698878-14-6 Metabolism Tyrosine Kinase/Adaptors CSF-1R NAMPT c-Fms PBEF Nampt IN 1 Visfatin inhibit LSN-3154567 Pre-B cell colony enhancing factor Nicotinamide phosphoribosyl transferase LSN 3154567 Inhibitor LSN3154567 NamptIN1 inhibitor