ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC 50 =1 nM; HCV GT1b EC 50 =0.3 nM).
性状
Solid
IC50 & Target[1][2]
NS5B polymerase
体外研究(In Vitro)
ABT-072 is a non-nucleoside NS5B polymerase inhibitor with nanomolar potency in vitro against genotype 1a and 1b hepatitis C virus polymerases. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ABT-072 (5 and/or 30 mg/kg; i.v. or p.o.) shows good PK properties.
ABT-072 (2.5 and/or 30 mg/kg; i.v. or p.o.) shows low plasma clearance and high oral bioavailability. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Lawitz E, et al. A phase 2a trial of 12-week interferon-free therapy with two direct-acting antivirals (ABT-450/r, ABT-072) and ribavirin in IL28B C/C patients with chronic hepatitis C genotype 1. J Hepatol. 2013;59(1):18-23.[2]. Shi Y, et al. Assessing Supersaturation and Its Impact on In Vivo Bioavailability of a Low-Solubility Compound ABT-072 With a Dual pH, Two-Phase Dissolution Method. J Pharm Sci. 2016;105(9):2886-2895.
溶解度数据
In Vitro: DMSO : 80 mg/mL (170.38 mM; Need ultrasonic)配制储备液
[1]. Lawitz E, et al. A phase 2a trial of 12-week interferon-free therapy with two direct-acting antivirals (ABT-450/r, ABT-072) and ribavirin in IL28B C/C patients with chronic hepatitis C genotype 1. J Hepatol. 2013;59(1):18-23.[2]. Shi Y, et al. Assessing Supersaturation and Its Impact on In Vivo Bioavailability of a Low-Solubility Compound ABT-072 With a Dual pH, Two-Phase Dissolution Method. J Pharm Sci. 2016;105(9):2886-2895.