Skip to main content
. 2013 Jul 22;4(9):846–851. doi: 10.1021/ml400176n

Table 6. Summary of in Vitro ADME/T Properties of NTR1 Agonist 32.

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