FKK6 is a selective agonist for pregnane X receptor ( PXR ) with an EC 50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS -induced colitis in mouse model [1] [2].
References:
[1]. Dvořák Z, et al., In vitro safety signals for potential clinical development of the anti-inflammatory pregnane X receptor agonist FKK6. Bioorg Chem. 2024 Mar;144:107137.
[2]. Dvořák Z, et al., Targeting the pregnane X receptor using microbial metabolite mimicry. EMBO Mol Med. 2020 Apr 7;12(4):e11621.
References:
[1]. Dvořák Z, et al., In vitro safety signals for potential clinical development of the anti-inflammatory pregnane X receptor agonist FKK6. Bioorg Chem. 2024 Mar;144:107137.
[2]. Dvořák Z, et al., Targeting the pregnane X receptor using microbial metabolite mimicry. EMBO Mol Med. 2020 Apr 7;12(4):e11621.