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Benzimidazole derivative XY123 is a potent, selective, and orally available RORγ inverse agonist. In this study, all liver microsome assays were performed by Medicilon

2023-07-11
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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. 


cancerinflammatorymetabolic-stabilitypharmacokinetics-propertyoral-bioavailabilityhalf-lifeliver-microsome-assay
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TAK-931 is a cancer therapeutic with a unique mechanism of action. Antitumor efficacy studies for TAK-931 were carried out at Medicilon
2023-08-21
Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell division cycle 7 (CDC7) has attracted attention as a target. Researchers have developed an oral CDC7-selective inhibitor, TAK-931, as a candidate clinical anticancer drug. TAK-931 demonstrated marked, dose-dependent antitumor activity, without severe body weight loss. Antitumor efficacy studies for TAK-931 were carried out in two pancreatic PDX models, PHTX-249Pa and PHTXM-97Pa, at Medicilon.
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The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
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RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).
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Address: 20 Maguire Road, Suite 103, Lexington, MA 02421(America)

Tel: +1(626)986-9880(U.S.)

Address: Allia Future Business Centre Kings Hedges Road Cambridge CB4 2HY, UK

Tel: 0044 7790 816 954 (Europe)

Email: marketing@medicilon.com

  

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Fax: +86 (21) 5859-6369

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