Figure 4
From: Discovery, optimization, and evaluation of non-bile acid FXR/TGR5 dual agonists
(a) FXR agonist activity of bicyclo[2.2.2]octane-isonicotinamide derivatives 20f–20v. Efficacy(%); % vs OCA 1 µM as 100%, OCA; 100% (1 µM), 13.3% (0.1 µM); (b) TGR agonist activity of bicyclo[2.2.2]octane-isonicotinamide derivatives 20f–20v. Efficacy(%); % vs INT-767 10 µM as 100%, INT-767 100% (10 µM), 25.5% (1 µM), 1.7% (0.1 µM). (c) Structures of bicyclo[2.2.2]octane-isonicotinamide derivatives 20f-20v.
