store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NITD008 (7-Deaza-2'-C-acetylene-adenosine) 是一种有效的和选择性的腺苷核苷抑制剂,是一种腺苷核苷类似物,具有广谱的抗病毒活性,抑制登革热病毒、动物杯状病毒和寨卡病毒。
产品描述 | NITD008 (7-Deaza-2'-C-acetylene-adenosine) is a potent and selective adenosine nucleoside inhibitor.NITD008 is an adenosine nucleoside analog with broad-spectrum antiviral activity that inhibits dengue, animal cupripoxvirus, and Zika virus. |
靶点活性 | HCV 1b:0.11 μM (EC50), DENV-2:0.64 μM (EC50) |
体外活性 | NITD008 exhibits potent inhibition against various viruses, including Dengue virus (DENV), West Nile virus, yellow fever virus, and Poissan virus. In the case of DENV-2, NITD008 inhibits the virus in a dose-responsive manner, with an EC50 value of 0.64 μM. Treatment with 9 μM of the compound results in a reduction in viral titer by >104-fold[1].Furthermore, NITD008 also demonstrates inhibitory activity against a luciferase-reporting replicon of hepatitis C virus (HCV, genotype 1b), a member of the genus Hepacivirus, with an EC50 value of 0.11 μM[1]. |
体内活性 |
NITD008, with good pharmacokinetic properties, is orally bioavailable. The formulation using 6 N HCl (1.5 equimolar amount), 1 N NaOH (pH adjusted to 3.5), and 100 mM citrate buffer (pH 3.5) yields the best pharmacokinetic parameters. Following intravenous (i.v.) injection, NITD008 demonstrates a high volume of distribution (3.71 L/kg) and low systemic clearance (31.11 mL/min per kg), resulting in a long elimination half-life (t1/2=4.99 h). After oral dosing, NITD008 is rapidly absorbed (time of peak plasma concentration=0.5 h), reaching a maximal plasma concentration of 3 μM, with a bioavailability of 48%. When administered immediately after viral infection, a dose of 1 mg/kg of NITD008 does not reduce mortality, but treatment with 3 mg/kg provides partial protection, and doses of ≥10 mg/kg completely protect infected mice from death. NITD008 effectively suppresses peak viremia, reduces cytokine elevation, and prevents mortality in the infected mice[1]. |
别名 | 7-Deaza-2'-C-acetylene-adenosine |
分子量 | 290.27 |
分子式 | C13H14N4O4 |
CAS No. | 1044589-82-3 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (172.25 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.4451 mL | 17.2253 mL | 34.4507 mL | 86.1267 mL |
5 mM | 0.689 mL | 3.4451 mL | 6.8901 mL | 17.2253 mL | |
10 mM | 0.3445 mL | 1.7225 mL | 3.4451 mL | 8.6127 mL | |
20 mM | 0.1723 mL | 0.8613 mL | 1.7225 mL | 4.3063 mL | |
50 mM | 0.0689 mL | 0.3445 mL | 0.689 mL | 1.7225 mL | |
100 mM | 0.0345 mL | 0.1723 mL | 0.3445 mL | 0.8613 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。
NITD008 1044589-82-3 Others NITD-008 NITD 008 7-Deaza-2'-C-acetylene-adenosine Inhibitor inhibitor inhibit