Description | Opaviraline (GW-420867X) is a potent reverse transcriptase inhibitor that inhibits Human immunodeficiency virus 1 and has the potential to treat HIV infection. |
In vivo | 系统性暴露于Opaviraline时,随着剂量的增加其浓度会降低,并表现出时间依赖性的药代动力学特性,这表明Opaviraline的吸收减少和/或清除增加。Opaviraline的血浆半衰期约为50小时,因其作用时间相对较长,适合每日一次给药。[1] |
Synonyms | GW420867X, GW-867, HBY-1293, GW867, GW-420867X |
molecular weight | 280.29 |
Molecular formula | C14H17FN2O3 |
CAS | 178040-94-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 10 mg/mL (35.68 mM) |
References | 1. Moore KH, et al. Pharmacokinetics and safety of escalating single and repeat oral doses of GW420867X, a novel non-nucleoside reverse transcriptase inhibitor. Eur J Clin Pharmacol. 2001;56(11):805-811. 2. Saparpakorn, et al. Systematic investigation on the binding of GW420867X as HIV-1 reverse transcriptase inhibitor. Monatsh Chem 2011;142, 961–971. 3. Drusano GL,et al. Rational dose selection for a nonnucleoside reverse transcriptase inhibitor through use of population pharmacokinetic modeling and Monte Carlo simulation. Antimicrob Agents Chemother. 2002;46(3):913-916. |