| Bioactivity | NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM. | ||||||||||||
| Target | EC50: 0.64 μM (DENV-2) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | NITD008 | ||||||||||||
| CAS | 1044589-82-3 | ||||||||||||
| Formula | C13H14N4O4 | ||||||||||||
| Molar Mass | 290.27 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Yin Z, et al. An adenosine nucleoside inhibitor of dengue virus. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20435-9. |