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  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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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].

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].

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
Molecular Weight

290.27

Formula

C₁₃H₁₄N₄O₄

CAS No.

1044589-82-3

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

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NITD008
Cat. No.:
HY-12957
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NITD008

Cat. No.: HY-12957