Bioactivity | ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM)[1][2][3]. | ||||||||||||
Target | NS5B polymerase | ||||||||||||
Invitro | ABT-072 is a non-nucleoside NS5B polymerase inhibitor with nanomolar potency in vitro against genotype 1a and 1b hepatitis C virus polymerases[1]. | ||||||||||||
In Vivo | ABT-072 (5 and/or 30 mg/kg; i.v. or p.o.) shows good PK properties[3].ABT-072 (2.5 and/or 30 mg/kg; i.v. or p.o.) shows low plasma clearance and high oral bioavailability[3]. Animal Model: | ||||||||||||
Name | ABT-072 | ||||||||||||
CAS | 1132936-00-5 | ||||||||||||
Formula | C24H27N3O5S | ||||||||||||
Molar Mass | 469.55 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. [3]. Randolph JT, et al. Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability. J Med Chem. 2018;61(3):1153-1163. |