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苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中，所有肝微粒体测定均通过美迪西进行

2023-07-05
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Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. XY123 potently inhibits the RORγ transcription activity with an IC50 value of 64 nM. XY123 demonstrates good metabolic stability and a pharmacokinetics property with reasonable oral bioavailability (32.41%) and moderate half-life (4.98 h). 

All liver microsome assays were performed by Medicilon.

49.pngReference:

Xishan Wu, et al. Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist. J Med Chem. 2021 Jun 24;64(12):8775-8797. doi: 10.1021/acs.jmedchem.1c00763. 

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