1. Anti-infection Cell Cycle/DNA Damage
  2. Dengue virus Flavivirus DNA/RNA Synthesis
  3. NITD008

NITD008  (Synonyms: 7-Deaza-2'-C-acetylene-adenosine)

目录号: HY-12957 纯度: 98.04%
COA 产品使用指南

NITD008是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0.64 μM。NITD008 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

NITD008 Chemical Structure

NITD008 Chemical Structure

CAS No. : 1044589-82-3

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850
In-stock
1 mg ¥1591
In-stock
5 mg ¥3500
In-stock
10 mg ¥5600
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM. NITD008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

EC50: 0.64 μM (DENV-2)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 CC50
> 100 μM
Compound: 1
Cytotoxicity against human A549 cells assessed as intracellular ATP level by Celltiter-Glo luminescent assay
Cytotoxicity against human A549 cells assessed as intracellular ATP level by Celltiter-Glo luminescent assay
[PMID: 20457821]
A549 CC50
> 50 μM
Compound: NITD008
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
[PMID: 35306290]
A549 EC50
0.46 μM
Compound: NITD008
Antiviral activity against Dengue virus 3 MY22366 infected in human A549 cells by CFI assay
Antiviral activity against Dengue virus 3 MY22366 infected in human A549 cells by CFI assay
[PMID: 20516277]
A549 EC50
0.7 μM
Compound: NITD008
Antiviral activity against Dengue virus 4 MY22713 infected in human A549 cells by CFI assay
Antiviral activity against Dengue virus 4 MY22713 infected in human A549 cells by CFI assay
[PMID: 20516277]
A549 EC50
0.7 μM
Compound: 1
Antiviral activity against at 0.3 MOI Dengue virus 2 infected in human A549 cells assessed as level of E protein after 48 hrs by ELISA
Antiviral activity against at 0.3 MOI Dengue virus 2 infected in human A549 cells assessed as level of E protein after 48 hrs by ELISA
[PMID: 20457821]
A549 EC50
1.12 μM
Compound: NITD008
Antiviral activity against Dengue virus 2 MY10340 infected in human A549 cells by CFI assay
Antiviral activity against Dengue virus 2 MY10340 infected in human A549 cells by CFI assay
[PMID: 20516277]
A549 EC50
1.64 μM
Compound: NITD008
Antiviral activity against Dengue virus 2 NGC infected in human A549 cells by CFI assay
Antiviral activity against Dengue virus 2 NGC infected in human A549 cells by CFI assay
[PMID: 20516277]
A549 EC50
2.61 μM
Compound: NITD008
Antiviral activity against Dengue virus 1 MY10245 infected in human A549 cells by CFI assay
Antiviral activity against Dengue virus 1 MY10245 infected in human A549 cells by CFI assay
[PMID: 20516277]
BHK-21 EC50
0.7 μM
Compound: 1
Antiviral activity against at 0.3 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as reduction in viral titer after 48 hrs postinfection
Antiviral activity against at 0.3 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as reduction in viral titer after 48 hrs postinfection
[PMID: 20457821]
HEK293 EC50
9.2 μM
Compound: 1
Antiviral activity against Dengue virus 2 infected in human HEK293 cells assessed as level of viral titer after 48 hrs by luciferase reporter gene assay in presence of siRNA targeting adenosine kinase
Antiviral activity against Dengue virus 2 infected in human HEK293 cells assessed as level of viral titer after 48 hrs by luciferase reporter gene assay in presence of siRNA targeting adenosine kinase
[PMID: 20457821]
Huh-7 EC50
0.2 μM
Compound: NITD-008
Antiviral activity against Zika virus H/PF/2013 infected in human HuH7 cells assessed as reduction in virus replication incubated for 24 hrs by plaque reduction assay
Antiviral activity against Zika virus H/PF/2013 infected in human HuH7 cells assessed as reduction in virus replication incubated for 24 hrs by plaque reduction assay
[PMID: 32435384]
Huh-7 EC50
1 μM
Compound: NITD-008
Antiviral activity against Dengue virus 2 EDEN 3295 infected in human HuH7 cells assessed as reduction in virus replication incubated for 48 hrs by plaque reduction assay
Antiviral activity against Dengue virus 2 EDEN 3295 infected in human HuH7 cells assessed as reduction in virus replication incubated for 48 hrs by plaque reduction assay
[PMID: 32435384]
Huh-7 CC50
100 μM
Compound: NITD-008
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescent assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescent assay
[PMID: 33208235]
Huh-7 CC50
100 μM
Compound: NITD-008
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter Glo Luminescent assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter Glo Luminescent assay
[PMID: 32435384]
PBMC EC50
0.58 μM
Compound: NITD008
Antiviral activity against Dengue virus 2 NGC infected in human PBMC cells by plaque assay
Antiviral activity against Dengue virus 2 NGC infected in human PBMC cells by plaque assay
[PMID: 20516277]
RD CC50
> 20 μM
Compound: 3; NITD008
Cytotoxicity against human RD cells assessed as reduction in cell viability by Cell Titer-Glo luminescent cell viability assay
Cytotoxicity against human RD cells assessed as reduction in cell viability by Cell Titer-Glo luminescent cell viability assay
[PMID: 34560428]
RD CC50
> 20 μM
Compound: 4; NITD008
Cytotoxicity against human RD cells infected with EV71 incubated for 3 days by CellTiter 96 luminescent cell viability assay
Cytotoxicity against human RD cells infected with EV71 incubated for 3 days by CellTiter 96 luminescent cell viability assay
[PMID: 35598412]
RD CC50
> 20 μM
Compound: 4; NITD008
Cytotoxicity against human RD cells infected with CA6 incubated for 3 days by CellTiter 96 luminescent cell viability assay
Cytotoxicity against human RD cells infected with CA6 incubated for 3 days by CellTiter 96 luminescent cell viability assay
[PMID: 35598412]
RD CC50
> 20 μM
Compound: 4; NITD008
Cytotoxicity against human RD cells infected with CA16 incubated for 3 days by CellTiter 96 luminescent cell viability assay
Cytotoxicity against human RD cells infected with CA16 incubated for 3 days by CellTiter 96 luminescent cell viability assay
[PMID: 35598412]
Vero CC50
> 100 μM
Compound: NITD008
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability treated for 3 days measured on day 4 by cell titer-blue fluorescent assay
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability treated for 3 days measured on day 4 by cell titer-blue fluorescent assay
[PMID: 26774922]
Vero EC50
0.03 μM
Compound: NITD008
Antiviral activity against clinical isolates of Dengue virus 4 Martinique 017 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
Antiviral activity against clinical isolates of Dengue virus 4 Martinique 017 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
[PMID: 26774922]
Vero EC50
0.08 μM
Compound: NITD008
Antiviral activity against clinical isolates of Dengue virus 4 Dakar HD34460 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
Antiviral activity against clinical isolates of Dengue virus 4 Dakar HD34460 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
[PMID: 26774922]
Vero EC50
0.12 μM
Compound: NITD008
Antiviral activity against clinical isolates of Dengue virus 3 Bolivia 4025 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
Antiviral activity against clinical isolates of Dengue virus 3 Bolivia 4025 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
[PMID: 26774922]
Vero EC50
0.67 μM
Compound: NITD008
Antiviral activity against EV71 infected in African green monkey Vero cells after 48 hrs by plaque assay
Antiviral activity against EV71 infected in African green monkey Vero cells after 48 hrs by plaque assay
[PMID: 27776325]
Vero EC50
0.82 μM
Compound: NITD008
Antiviral activity against clinical isolates of Dengue virus 2 Martinique H/IMTSSA-MART/98-703 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
Antiviral activity against clinical isolates of Dengue virus 2 Martinique H/IMTSSA-MART/98-703 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
[PMID: 26774922]
Vero EC50
0.86 μM
Compound: NITD008
Antiviral activity against clinical isolates of Dengue virus 1 Indonesia JKT 1186 TVP 949 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
Antiviral activity against clinical isolates of Dengue virus 1 Indonesia JKT 1186 TVP 949 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method
[PMID: 26774922]
Vero CC50
119.97 μM
Compound: NITD008
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
[PMID: 27776325]
Vero EC50
137 nM
Compound: 3; NITD008
Inhibition of RNA-dependent RNA polymerase in Zika virus GZ01/2016 infected in African green monkey Vero cells assessed as antiviral activity by measuring viral RNA by RT-qPCR method
Inhibition of RNA-dependent RNA polymerase in Zika virus GZ01/2016 infected in African green monkey Vero cells assessed as antiviral activity by measuring viral RNA by RT-qPCR method
[PMID: 31549836]
Vero EC50
137 nM
Compound: 3; NITD008
Inhibition of RNA-dependent RNA polymerase in Zika virus FSS13025/2010 infected in African green monkey Vero cells assessed as antiviral activity by measuring viral RNA by RT-qPCR method
Inhibition of RNA-dependent RNA polymerase in Zika virus FSS13025/2010 infected in African green monkey Vero cells assessed as antiviral activity by measuring viral RNA by RT-qPCR method
[PMID: 31549836]
Vero EC50
137 nM
Compound: 3; NITD008
Inhibition of RNA-dependent RNA polymerase in Zika virus GZ01/2016 infected in African green monkey Vero cells assessed as antiviral activity measured 48 hrs post infection by plaque assay
Inhibition of RNA-dependent RNA polymerase in Zika virus GZ01/2016 infected in African green monkey Vero cells assessed as antiviral activity measured 48 hrs post infection by plaque assay
[PMID: 31549836]
Vero EC50
137 nM
Compound: 3; NITD008
Inhibition of RNA-dependent RNA polymerase in Zika virus FSS13025/2010 infected in African green monkey Vero cells assessed as antiviral activity measured 48 hrs post infection by plaque assay
Inhibition of RNA-dependent RNA polymerase in Zika virus FSS13025/2010 infected in African green monkey Vero cells assessed as antiviral activity measured 48 hrs post infection by plaque assay
[PMID: 31549836]
Vero CC50
74 μM
Compound: NITD008
Cytotoxicity against African green monkey Vero cells incubated for 48 hrs by DAPI staining based assay
Cytotoxicity against African green monkey Vero cells incubated for 48 hrs by DAPI staining based assay
[PMID: 36596229]
体外研究
(In Vitro)

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 0.64 μM; treatment with 9 μM compound reduces viral titer by >104-fold[1]. 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 0.11 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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 100 mM 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 (31.11 mL/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 3 μM 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 ≥10 mg/kg completely protects the infected mice from death. NITD008 can suppress peak viremia, decrease cytokine elevation, and prevent death[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

290.27

Formula

C13H14N4O4

CAS 号
性状

固体

颜色

White to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 50 mg/mL (172.25 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4451 mL 17.2253 mL 34.4507 mL
5 mM 0.6890 mL 3.4451 mL 6.8901 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.61 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.61 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.04%

参考文献
Cell Assay
[1]

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, 50 μM) for 48 h; cell viability is quantified using a MTT assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

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 0.2 mL of RPMI-1640 medium containing 3×107 pfu/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, 50 mg/kg) in 0.2-0.25 mL of formulation solution is administered by p.o. gavage. The mice (6 or 8 mice per group) are monitored twice a day[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 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 0.6890 mL 3.4451 mL 6.8901 mL 17.2253 mL
10 mM 0.3445 mL 1.7225 mL 3.4451 mL 8.6127 mL
15 mM 0.2297 mL 1.1484 mL 2.2967 mL 5.7418 mL
20 mM 0.1723 mL 0.8613 mL 1.7225 mL 4.3063 mL
25 mM 0.1378 mL 0.6890 mL 1.3780 mL 3.4451 mL
30 mM 0.1148 mL 0.5742 mL 1.1484 mL 2.8709 mL
40 mM 0.0861 mL 0.4306 mL 0.8613 mL 2.1532 mL
50 mM 0.0689 mL 0.3445 mL 0.6890 mL 1.7225 mL
60 mM 0.0574 mL 0.2871 mL 0.5742 mL 1.4354 mL
80 mM 0.0431 mL 0.2153 mL 0.4306 mL 1.0766 mL
100 mM 0.0345 mL 0.1723 mL 0.3445 mL 0.8613 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NITD008
目录号:
HY-12957
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