中文名 | 7-脱氮-2'-C-乙炔腺苷 |
英文名 | 7-Deaza-2'-C-ethynyladenosine |
别名 | 化合物 T16325 7-脱氮-2'-C-乙炔腺苷 |
英文别名 | 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 |
化学式 | C13H14N4O4 |
分子量 | 290.28 |
密度 | 1?+-.0.1 g/cm3(Predicted) |
沸点 | 631.8±55.0 °C(Predicted) |
酸度系数 | 10.48±0.70(Predicted) |
存储条件 | Room Temprature |
体外研究 | 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. |
体内研究 | 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. |
上游原料 | Methyl 3,5-di-O-(2,4-dichlorobenzyl)-D-ribofuranoside |
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