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Figure 1.
In vitro characterization of A1120. A, chemical structure of
A1120. B–D, representative radioligand binding isotherms for
human RBP4 (B), mouse RBP4 (C), and human CRBP1 (D). In each
case, [^3H]retinol was used as the radioligand. IC[50] values
were 90 nm for hRBP4 (n = 11 independent determinations), 66 nm
for mRBP4 (n = 4), and > 30 μm for hCRBP1 (n = 4). E,
concentration-response curves in the FRET assay. Retinol was
dosed in the presence of RBP4, TTR, and increasing
concentrations of A1120 (0–1 × 10^-5 m, as shown on the
right side). The K[i] of A1120 was 8.3 nm (n = 3).
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