Table 2Summary of in vitro ADME properties of ML317

Aqueous Solubilitya

(μg/mL, μM)
Assay Media Solubilityb

(μg/mL, μM)
PAMPA Pec

(x10−6 cm/s @ Donor pH)
Plasma Protein Binding
(% Bound)
Plasma Stabilityd

Human Mouse/1:1 Plasma:PBS
Hepatic Microsome Stabilitye

Human/Mouse
Hepatic Toxicityf

LC50 (μM)
Human

1μM/10μM
Mouse

1μM/10μM
93/22968/16914 @ 5.0
209 @ 6.2
52 @ 7.4
99.68/99.8598.97/99.3195.3/78.489.6/74.326
a

in 1x PBS, pH 7.4

b

in Luria-Bertani broth (10g tryptone, 5g yeast extract, 10g NaCl)

c

in aqueous buffer (pION),; Donor compartment pH 5.0/6.2/7.4; Acceptor compartment pH 7.4 @ RT

d

% remaining at 3 hr @ 37°C

e

% remaining at 1 hr @ 37°C

f

towards Fa2N-4 immortalized human hepatocytes

From: 3-(2,6-difluorobenzamido)-5-(4-ethoxyphenyl) thiophene-2-carboxylic acid inhibits E.coli UT189 bacterial capsule biogenesis

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