Synonyms: compound 11c [PMID: 36318660]
Compound class:
Synthetic organic
Comment: TP0472993 (11c) is an inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2 isozymes [2]. It inhibits production of the arachidonic acid metabolite 20-HETE. Reducing the circulating 20-HETE level is predicted to have anti-fibrotic activity that provides a renoprotective mechanism in chronic kidney disease progression [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. Hirata T, Ohara H, Kojima N, Koretsune H, Hasegawa Y, Inatani S, Takahashi T. (2023)
Renoprotective Effect of TP0472993, a Novel and Selective 20-Hydroxyeicosatetraenoic Acid Synthesis Inhibitor, in Mouse Models of Renal Fibrosis. J Pharmacol Exp Ther, 386 (1): 56-69. [PMID:37142440] |
2. Kawamura M, Kobashi Y, Tanaka H, Bohno-Mikami A, Hamada M, Ito Y, Hirata T, Ohara H, Kojima N, Koretsune H et al.. (2022)
Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition. J Med Chem, 65 (21): 14599-14613. [PMID:36318660] |