TKB272 

TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC₅₀ of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC₅₀ as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC₅₀ of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection^[1].

653.69

C₃₀H₃₅F₄N₅O₅S

2892688-18-3

O=C(N[C@H](C(N1C[C@H](C2(C)C)[C@H]2[C@H]1C(N[C@H](C(C3=NC(C=C(F)C=C4)=C4S3)=O)C[C@@H]5CCNC5=O)=O)=O)C(C)(C)C)C(F)(F)F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Higashi-Kuwata N, et al. An orally available P1'-5-fluorinated M inhibitor blocks SARS-CoV-2 replication without booster and exhibits high genetic barrier. PNAS Nexus. 2025 Jan 7;4(1):pgae578.  [Content Brief]