Steady state studies varying NADPH and inhibitor concentrations indicate that treatment with the fast inhibitors 7 and 8 or the slow inhibitor 3 , (the only slow inhibitor reaching equilibrium in 6 h), resulted in decreases in both K m and V max values consistent with uncompetitive inhibition of TGR, while treatment with 9 , a close analog of compound 8 synthesized ad hoc to facilitate structural studies (see below), changed only the V max indicating noncompetitive inhibition (Supplementary Tables 15 and 16)
Food in the stomach does not affect subcutaneous absorption
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Cadet, J., Angelov, D., Di Mascio, P., & Wagner, J
Exposure to pro-oxidant stimuli usually induces Nrf2 activation and upregulation of antioxidant enzyme expression through binding to the antioxidant response element (ARE), localized in the antioxidant enzyme gene promoters