| aqueous solubility
(μM) in pION buffer; pH 5.0/6.2/7.4 |
>297/21.4/1.2 |
| aqueous solubility
(μM) in 1× PBS, pH 7.4 |
1.1 |
| PAMPA permeability, Pe (× 10–6 cm/s), donor pH: 5.0/6.2/7.4, acceptor
pH: 7.4 |
1163/2145/2093 |
| BBB-PAMPA
permeability, Pe (× 10–6 cm/s), donor pH: 7.4,
acceptor pH: 7.4 |
399 |
| plasma protein
binding (% bound) |
human 1 μM/10 μM |
99.5/99.2 |
| mouse 1 μM/10 μM |
99.7/98.9 |
| plasma stability
(% remaining at 3 h) human/mouse |
100/99.6 |
| hepatic microsome stability (% remaining
at 1 h) human/mouse |
1.4/0.2 |
| toxicity toward Fa2N-4 immortalized
human hepatocytes over 24 h, LC50 (μM) |
29.6 |