For research use only. Not for therapeutic Use.
AVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC50=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV)[1][2].
AVG-233 (1-100 μM) blocks 3´RNA extension elongation but does not interfere with 3´RNA extension by up to three nucleotides after de novo initiation from the promoter or back-priming[1].
AVG-233 (20 μM) reduces virus yield of RSV A2-L19F (EC50=0.31 μM), RSV strain 2-20 (EC50=0.14 μM) and RSV clinical isolate 718 (EC50=0.2 μM) [1].
AVG-233 (1.25-40 μM; 0-300 s) suppresses RNA synthesis by the L1-1749 fragment in a dose-dependent manner with an IC50 value of 13.7 μM. AVG-233 bounds L and the L1-1749 fragment with similar affinities (dissociation constants (KD’s) are 38.3 μM and 53.1 μM, respectively)[2].
AVG-233 (50-100 mg/kg; i.g.; once) decreases lung viral load in the RSV mouse model[2].
AVG-233 (2-20 mg/kg; i.v. and p.o.; once; male CD-1 mice) has good orally bioavailable and the maximum plasma concentration about 2 μM[1].
| Catalog Number | I042960 |
| CAS Number | 2151937-80-1 |
| Synonyms | 5-[(6-chloropyridin-2-yl)methyl]-1-[(4-methoxyphenyl)methyl]-4-methyl-2-pyridin-2-ylpyrazolo[4,3-c]pyridine-3,6-dione |
| Molecular Formula | C26H22ClN5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H22ClN5O3/c1-17-25-21(14-24(33)30(17)16-19-6-5-7-22(27)29-19)31(15-18-9-11-20(35-2)12-10-18)32(26(25)34)23-8-3-4-13-28-23/h3-14H,15-16H2,1-2H3 |
| InChIKey | CXZZYJLIYWCICH-UHFFFAOYSA-N |
| SMILES | CC1=C2C(=CC(=O)N1CC3=NC(=CC=C3)Cl)N(N(C2=O)C4=CC=CC=N4)CC5=CC=C(C=C5)OC |
| Reference | [1]. Cox RM, et, al. Development of an allosteric inhibitor class blocking RNA elongation by the respiratory syncytial virus polymerase complex. J Biol Chem. 2018 Oct 26;293(43):16761-16777. [2]. Sourimant J, et, al. Orally efficacious lead of the AVG inhibitor series targeting a dynamic interface in the respiratory syncytial virus polymerase. Sci Adv. 2022 Jun 24;8(25):eabo2236. |
