Identification | Back Directory | [Name]
ABT-072 | [CAS]
1132936-00-5 | [Synonyms]
ABT-072 ABT-072
(ABT072) (E)-N-(4-(3-(tert-Butyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxystyryl)phenyl)methanesulfonamide Methanesulfonamide, N-[4-[(1E)-2-[5-(3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinyl)-3-(1,1-dimethylethyl)-2-methoxyphenyl]ethenyl]phenyl]- | [Molecular Formula]
C24H27N3O5S | [MOL File]
1132936-00-5.mol | [Molecular Weight]
469.55 |
Chemical Properties | Back Directory | [density ]
1.310±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
8.46±0.10(Predicted) | [color ]
Off-white to yellow |
Hazard Information | Back Directory | [Uses]
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]. | [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: | Rats[3] | Dosage: | 5 and/or 30 mg/kg (Pharmacokinetic Analysis) | Administration: | I.v. or p.o. | Result: | Showed good PK properties.
|
Animal Model: | Dog[3] | Dosage: | 2.5 or 30 mg/kg (Pharmacokinetic Analysis) | Administration: | I.v. or p.o. | Result: | Showed low plasma clearance and high oral bioavailability.
|
| [storage]
Store at -20°C | [References]
[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. DOI:10.1016/j.jhep.2013.02.009 [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. DOI:10.1016/j.xphs.2016.04.036 [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. DOI:10.1021/acs.jmedchem.7b01630 |
|
Company Name: |
BOC Sciences
|
Tel: |
1-631-485-4226; 16314854226 |
Website: |
https://www.bocsci.com |
Company Name: |
InvivoChem
|
Tel: |
13549236410 |
Website: |
https://www.invivochem.cn/ |
|