NITD008 is an effective and selective flaviviruse inhibitor that can inhibit Dengue Virus Type 2 (EC50: 0.64 μM).

NITD008 also inhibits a luciferase-reporting replicon of the hepatitis C virus (HCV, genotype 1b), a member from the genus Hepacivirus (EC50: 0.11 μM). NITD008 potently inhibits others, including Dengue virus (DENV), West Nile virus, yellow fever virus, and Poisson virus. NITD008 treatment with 9 μM compound reduces viral titer by >104-fold .

NITD008 is orally bioavailable and has good pharmacokinetic properties. NITD008 can suppress peak viremia, decrease cytokine elevation, and prevent death. 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), NITD008 shows the best pharmacokinetic parameters. After NITD008 (p.o.) treatment, is rapidly absorbed (time of peak plasma concentration=0.5 h), with a maximal plasma concentration of 3 μM and bioavailability of 48%. Following NITD008 ( i.v. injection) has a high volume of distribution (3.71 L/kg) and a low systemic clearance (31.11 mL/min per kg), causing a long elimination half-life (t1/2=4.99 h). 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 .

1044589-82-3

C13H14N4O4

290.27

7-Deaza-2'-C-acetylene-adenosine;NITD008

DMSO:50 mg/mL (172.25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years