AVG-233 是一种口服有效的 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。AVG-233 阻止启动子上的病毒聚合酶复合物的启动。AVG-233 结合位点存在于 L_1-1749 片段中。AVG-233 对 RSV 毒株和临床分离株均具有纳摩尔活性 (EC₅₀=0.14-0.31 μM)。AVG-233 可用于呼吸道合胞病毒 (RSV) 研究。

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 L 1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC 50 =0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV).

Solid

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.
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) .
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).
has not independently confirmed the accuracy of these methods. They are for reference only.

AVG-233 (50-100 mg/kg; i.g.; once) decreases lung viral load in the RSV mouse model.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[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.

In Vitro: DMSO : 50 mg/mL (102.47 mM; ultrasonic and warming and heat to 60°C)配制储备液