中文名称: | NITD008 | ||||
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英文名称: | NITD008 | ||||
别名: | 7-Deaza-2'-C-acetylene-adenosine | ||||
CAS No: | 1044589-82-3 | 分子式: | C13H14N4O4 | 分子量: | 290.27 |
CAS No: | 1044589-82-3 | ||||
分子式: | C13H14N4O4 | ||||
分子量: | 290.27 |
基本信息
产品编号:N10445 |
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产品名称:NITD008 |
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CAS: |
1044589-82-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
290.27 |
-20℃ |
一个月 |
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化学名: |
(2R,3R,4R,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-(hydroxymethyl)oxolane-3,4-diol |
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Solubility (25°C) |
体外 |
DMSO |
≥50mg/mL (172.25mM) |
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Ethanol |
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Water |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.4451mL |
17.2253mL |
34.4507mL |
5mM |
0.6890mL |
3.4451mL |
6.8901mL |
10mM |
0.3445mL |
1.7225mL |
3.4451mL |
生物活性
产品描述 |
一种有效的和选择性的黄病毒 (flaviviruses) 抑制剂,抑制登革热病毒2型 (Dengue Virus Type 2 (DENV-2)) 的 EC50 值为0.64μM。 |
靶点/IC50 |
EC50: 0.64μM (DENV-2) |
体外研究 |
NITD008 potently inhibits other, including Dengue virus (DENV), West Nile virus, yellow fever virus, and Poissan virus. NITD008 inhibits DENV-2 in a dose-responsive manner, with an EC50 value of 0.64μM; treatment with 9μM compound reduces viral titer by >104-fold. NITD008 also inhibits a luciferase-reporting replicon of hepatitis C virus (HCV, genotype 1b), a member from the genus Hepacivirus, with an EC50 value of 0.11μM. |
体内研究 |
NITD008 is orally bioavailable and has good pharmacokinetic properties. NITD008 exhibits the best pharmacokinetic parameters when formulated using 6 N of HCl (1.5 equimolar amount), 1 N of NaOH (pH adjusted to 3.5), and 100mM citrate buffer (pH 3.5). Following i.v. injection, NITD008 has a high volume of distribution (3.71 L/kg) and a low systemic clearance(31.11mL/min per kg), resulting in a long elimination half-life (t1/2=4.99 h). After p.o. dosing, NITD008 is rapidly absorbed(time of peak plasma concentration=0.5 h), with a maximal plasma concentration of 3μM and bioavailability of 48%. Treatment of the mice immediately after viral infection with 1 mg/kg of NITD008 does not reduce mortality, but treatment with 3 mg/kg partially protects and treatment with ≥10mg/kg completely protects the infected mice from death. NITD008 can suppress peak viremia, decrease cytokine elevation, and prevent death.
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推荐实验方法(仅供参考)
细胞实验: |
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Cell Assay |
For measurement of compound cytotoxicity, Vero cells (10000 cells per well of a 96-well plate) are incubated with various concentrations of NITD008 (3, 6, 12, 25, 50μM) for 48 h; cell viability is quantified using a MTT assay . |
动物实验: |
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Animal Administration |
Mice The in vivo efficacy of NITD008 is evaluated in a dengue viremia model and a lethal model in mice. Both models use AG129 mice (with knockout IFN-α/β and IFN-γ receptors). DENV-2 strains TSV01and D2S10, respectively, are used in the 2 models and are propagated in C6/36 mosquito cells grown in RPMI-1640 medium with 5% FBS (vol/vol) at 28°C. The evaluation in the lethal model is performed by injecting mice i.v. with 0.2mL of RPMI-1640 medium containing 3×107pfu/mL DENV-2 strain D2S10; the infected mice are then subjected to different treatment regimens, as indicated in each experiment. NITD008 (1, 3, 10, 25, 50mg/kg) in 0.2-0.25mL of formulation solution is administered by p.o. gavage. The mice (6 or 8 mice per group) are monitored twice a day. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )