中文名称: NITD008
英文名称: NITD008
CAS No: 1044589-82-3
分子式: C13H14N4O4
分子量: 290.27
N10445 NITD008 ≥98% (psaitong)
包装规格:
1mg 5mg in glass bottle
溶解性:
溶于DMSO(≥ 50 mg/mL)
产品描述:

基本信息

产品编号:N10445

产品名称:NITD008

CAS:

1044589-82-3

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C13H14N4O4

溶于液体

-80℃

六个月

分子量

290.27

-20℃

一个月

化学名: 

(2R,3R,4R,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-(hydroxymethyl)oxolane-3,4-diol

 

Solubility (25°C)

 

体外

DMSO

≥50mg/mL (172.25mM)

Ethanol

 

Water

 

体内

现配现用

 

1mg/ml表示微溶或不溶。

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。

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.

 

 

推荐实验方法(仅供参考)

细胞实验:

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:

 

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):