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. 2018 May 21;9(6):1069–1075. doi: 10.1039/c8md00204e

Table 3. In vitro pharmacokinetic profile of 7.

Test Comp. 7
Effect of HSA
5-HT2B IC50 14.1
5-HT2B IC50 + 4% HSA 18.7
Stability in simulated fluids (t1/2, min)
Gastric (pH 1.6) 259
Intestinal (pH 6.5) >500
Stability in human plasma (% remaining at 120 min) 97.4
CACO cell permeability
P app, A → B (10–6 cm s–1) 16.3
P app, B → A (10–6 cm s–1) 32.8
Stability in rat liver microsomes (t1/2, min) 179
Cytotoxicity in HepG2 cells (IC50, μM) >50