In Vitro Metabolic Profiling

GRL0617 (CAS no. 1093070-16-6) was obtained from Bio-Techne GmbH (Wiesbaden, Germany), and HY-17542 (1093070-14-4) was obtained from MedChemExpress LLC (Monmouth Junction, NJ, United States). Pooled HLMs (UltraPool HLM 150) were purchased from Corning (Woburn, MA, United States). Formic acid, NADPH, DMSO, and formaldehyde were purchased from Sigma Aldrich (St. Louis, MO, United States). All other reagents and chemicals were of the highest grade available commercially. Control, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, CYP3A4, and CYP3A5 recombinant CYP bactosomes, carboxylesterase (CES) 1 and CES2 were purchased from Cypex (Dundee, UK). Silensome control, Silensome CYP2D6 and Silensome CYP3A4 were purchased from Biopredic international (Saint Grégoire, France).

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Cho H., Kim Y.J., Chae J.W., Meyer M.R., Kim S.K, & Ryu C.S. (2023). In vitro metabolic characterization of the SARS-CoV-2 papain-like protease inhibitors GRL0617 and HY-17542. Frontiers in Pharmacology, 14, 1067408.

Publication 2023

UltraPool HLM 150) Formic acid NADPH DMSO formaldehyde

Carboxylesterase Ces2 Cyp1a2 Cyp2a6 Cyp2c8 Cyp2d6 Cyp2e1 Cyp3a4 Cyp3a5 Dmso Formaldehyde Formic acid Grl0617 Nadph

Corresponding Organization : Chungnam National University

Other organizations : Saarland University

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Variable analysis

independent variables

GRL0617 (CAS no. 1093070-16-6) obtained from Bio-Techne GmbH (Wiesbaden, Germany)
HY-17542 (1093070-14-4) obtained from MedChemExpress LLC (Monmouth Junction, NJ, United States)

dependent variables

Not explicitly mentioned

control variables

Formic acid, NADPH, DMSO, and formaldehyde purchased from Sigma Aldrich (St. Louis, MO, United States)
Pooled HLMs (UltraPool HLM 150) purchased from Corning (Woburn, MA, United States)
Control, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, CYP3A4, and CYP3A5 recombinant CYP bactosomes, carboxylesterase (CES) 1 and CES2 purchased from Cypex (Dundee, UK)
Silensome control, Silensome CYP2D6 and Silensome CYP3A4 purchased from Biopredic international (Saint Grégoire, France)

positive controls

Control, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, CYP3A4, and CYP3A5 recombinant CYP bactosomes, carboxylesterase (CES) 1 and CES2 purchased from Cypex (Dundee, UK)
Silensome control, Silensome CYP2D6 and Silensome CYP3A4 purchased from Biopredic international (Saint Grégoire, France)

negative controls

Silensome control purchased from Biopredic international (Saint Grégoire, France)

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