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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Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon

2023-07-11

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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).

Reference:

Zhanhui Li, et al. Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. Eur J Med Chem. 2022 Jan 15;228:114036. doi: 10.1016/j.ejmech.2021.114036.