Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHS-828 (GMX1778) 是一种竞争性的烟酰胺磷酸化转移酶抑制剂,IC50值 <25 nM。它通过降低细胞中的 NAD+水平发挥细胞毒性作用,具有抗癌活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 193 | 现货 | ||
5 mg | ¥ 412 | 现货 | ||
10 mg | ¥ 661 | 现货 | ||
25 mg | ¥ 1,394 | 现货 | ||
50 mg | ¥ 2,234 | 现货 | ||
100 mg | ¥ 3,578 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 453 | 现货 |
产品描述 | CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM). |
靶点活性 | NAMPT:<25 nM |
体外活性 | GMX1778 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. [1] GMX1778 induces programmed cell death with apoptotic features. [2] GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM). [3] |
体内活性 | GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice. [4] |
激酶实验 | In vitro coupled-enzyme NAMPT assay: Recombinant NAMPT activity is assessed using a coupled-enzyme assay based on the quantitation of NAD+. Reactions are performed at room temperature for 180 min using mixtures consisting of 50 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 0.5 mM β-mercaptoethanol, 0.005% bovine serum albumin, 1% DMSO, 2.0 U/ml lactate dehydrogenase, 4 mM sodium L-lactate, 0.4 U/ml diaphorase, 6 μΜ resazurin sodium salt, 0.4 mM PRPP, 3.0 nM NMNAT1, 125 μM ATP, 50 μM NM, and 2 to 5 μM recombinant NAMPT. Fluorescence s measured with a Tecan Safire plate reader (excitation wavelength, 560 nm; emission wavelength, 590 nm). Ki values are calculated using Graphpad Prism 4.0 software and the Cheng-Prusoff equation. |
细胞实验 | Serial dilutions of GMX1778 in DMSO are performed to achieve a final concentration of 0.2% DMSO. Relative ATP levels after 72 h are determined using a ViaLight HS high-sensitivity cytotoxicity and cell proliferation BioAssay kit per the manufacturer's instructions. For GMX1778 cytotoxicity rescue experiments, cells are treated with NA (10 μM) or NMN (100 μM) simultaneously with GMX1778. Sigmoidal dose-response curves are generated by nonlinear regression analysis of variable slope using GraphPad Prism version 4.00 (GraphPad Software) to calculate 50% inhibitory (IC50) values.(Only for Reference) |
别名 | CHS 828, GMX1778 |
分子量 | 371.86 |
分子式 | C19H22ClN5O |
CAS No. | 200484-11-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 69 mg/mL (185.6 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL | 67.2296 mL |
5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL | 13.4459 mL | |
10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL | 6.723 mL | |
20 mM | 0.1345 mL | 0.6723 mL | 1.3446 mL | 3.3615 mL | |
50 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL | 1.3446 mL | |
100 mM | 0.0269 mL | 0.1345 mL | 0.2689 mL | 0.6723 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。
CHS-828 200484-11-3 Apoptosis Metabolism NAMPT Nicotinamide phosphoribosyl transferase CHS828 inhibit PBEF Visfatin Inhibitor GMX 1778 Pre-B cell colony enhancing factor GMX-1778 CHS 828 GMX1778 inhibitor