Telaprevir-d4

Telaprevir-d4

• UNSPSC Description: Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
• Target Antigen: HCV; HCV Protease; Isotope-Labeled Compounds; SARS-CoV
• Type: Isotope-Labeled Compounds
• Related Pathways: Anti-infection;Metabolic Enzyme/Protease;Others
• Field of Research: Infection
• Solubility: 10 mM in DMSO
• Smiles: O=C(NC1C([2H])([2H])C1([2H])[2H])C([C@H](CCC)NC([C@@H]2[C@]3([H])[C@](CCC3)([H])CN2C([C@H](C(C)(C)C)NC([C@H](C4CCCCC4)NC(C5=NC=CN=C5)=O)=O)=O)=O)=O
• Molecular Weight: 683.87
• References & Citations: [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Lin K, et al. VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCv replicon cells. Antimicrob Agents Chemother. 2006 May;50(5):1813-22.|[3]Perni RB, et al. Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease. Antimicrob Agents Chemother. 2006 Mar;50(3):899-909.|[4]Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065.|[5]Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported