1. Cell Cycle/DNA Damage
    Anti-infection
  2. DNA/RNA Synthesis
    Influenza Virus
  3. NITD008

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

Cat. No.: HY-12957 Purity: >98.0%
Handling Instructions

NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM.

For research use only. We do not sell to patients.

NITD008 Chemical Structure

NITD008 Chemical Structure

CAS No. : 1044589-82-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 511 In-stock
Estimated Time of Arrival: December 31
1 mg USD 160 In-stock
Estimated Time of Arrival: December 31
5 mg USD 720 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM.

IC50 & Target

EC50: 0.64 μM (DENV-2)[1]

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.

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.

Molecular Weight

290.27

Formula

C₁₃H₁₄N₄O₄

CAS No.

1044589-82-3

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (172.25 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.3445 mL 1.7225 mL 3.4451 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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.

References
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Keywords:

NITD0087-Deaza-2'-C-acetylene-adenosineNITD 008NITD-008DNA/RNA SynthesisInfluenza VirusInhibitorinhibitorinhibit

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