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. 2014 Oct 6;35(11):1463–1472. doi: 10.1038/aps.2014.97

Table 2. TGR5 and FXR activities of triterpenoids. Data are presented as mean±SEM (n=3).

Name TGR5
FXR
EC50/nmol·L−1 Efficacy EC50/nmol·L−1
GW4064 48.82±0.4
INT-777 469.0±94.3 100.0±0.7 NR
577.4±86.3 89.77±1.2 NR
7082±453.6 87.67±1.3 NR
3190±443.8 90.19±1.3 NR
3979±994.1 93.04±0.8 NR
11α 237.8±73.6 91.63±0.4 NR
11β 1867±432.9 84.03±1.5 NR

EC50 and efficacy generated from human TGR5-based cAMP assay or human FXR-based reporter assay. NR=No response at concentrations up to 100 μmol/L.