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. 2022 May 17;11(10):1667. doi: 10.3390/cells11101667

Table 1.

In vitro profiling of ZED1227.

Molecular Mass [g/mol] 528.6
Solubility at pH 7.4
Solubility at pH 1.1
100 μM/0.05 g/L
48,900 μM/25.9 g/L
LogD (octanol/PBS pH 7.4) 2.0
Stability in PBS/saline (24 h, 37 °C) 10% at pH 7.4
89% at pH 5.0
Stability in artificial gastric and
intestinal fluid (24 h, 37 °C)
95%, simulated gastric fluid (pH 1.2)
82%, simulated intestinal fluid (pH 6.5)
A-B permeability (Caco-2-assay) Papp < 1 × 10−6 cm/s
Cytotoxicity
Proliferation: Caco-2 cells
      Huh7 cells
  Viability: Caco-2 cells
      Huh7 cells

no effect up to 1,000 μM
no effect up to 1,000 μM
no effect up to 1,000 μM
no effect up to 1,000 μM
Reactivity towards excess
glutathione (25 °C)
98% parent drug compound recovery
(after 48 h)