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Although the maximum plasma concentration is lower when compound 2 is administered PO (0.77 M) instead of IP (4.8 M), it is still 4.3-fold higher than LD 50 for ex vivo NTS determined in the commonly used 72 h assay, also indicating that TGR inhibitor 2 is orally bioavailable and the initial prediction of oral bioavailability based on the Lipinski et al

However, collection of high-quality evidence, such as that from double-blind placebo-controlled trials, on the efficacy of these compounds is a slow and arduous process