NITD008
7-Deaza-2'-C-ethynyladenosine
CAS: 1044589-82-3
Molecular Formula: C13H14N4O4
NITD008 - Names and Identifiers
| Name | 7-Deaza-2'-C-ethynyladenosine |
| Synonyms | NITD008 7-Deaza-2'-C-ethynyladenosine 7-Deaza-2'-C-acetylene-adenosine 7-(2-C-Ethynyl-β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-(2-C-ethynyl-β-D-ribofuranosyl)- (2R,3R,4R,5R)-2-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-(hydroxymethyl)tetrahydrofuran-3,4-diol |
| CAS | 1044589-82-3 |
NITD008 - Physico-chemical Properties
| Molecular Formula | C13H14N4O4 |
| Molar Mass | 290.28 |
| Density | 1?+-.0.1 g/cm3(Predicted) |
| Boling Point | 631.8±55.0 °C(Predicted) |
| pKa | 10.48±0.70(Predicted) |
| Storage Condition | Room Temprature |
| In vitro study | 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 EC 50 value of 0.64 μM; treatment with 9 μM compound reduces viral titer by >104-fold. NITD008 also inhibits a luciferase-reporting replicon of hepatitis C virus (HCV, genotype 1b), a member from the genus Hepacivirus, with an EC 50 value of 0.11 μM. |
| In vivo study | 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 (t 1/2 =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. |
NITD008 - References
| biological activity | NITD008 is a potent and selective yellow Virus (flaviviruses) inhibitor, the EC50 value for Dengue Virus Type 2 Virus (DENV-2) was 0.64 μm. |
| Target | EC50: 0.64 μm (DENV-2) |
Last Update：2024-04-09 20:52:54
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CAS: 1044589-82-3
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