TABLE 1

Binding affinities of ARBs against PPARγ assessed by isothermal titration calorimetry

The binding affinities (Kd = 1/Ka) were determined at 25°C by isothermal titration calorimetry. The PPARγ solution (approximately 25 μM) in the calorimetric cell was titrated with ARB solutions (1.4 μl per injection of 250 μM–3 mM) dissolved in the same buffer (PBS, pH 7.4 with 5% DMSO). Data are expressed as mean ± S.E.M. from independent triplicate experiments.

CompoundKd
μM
Telmisartan0.34 ± 0.04
Irbesartan10.3 ± 1.5
Azilsartan>100
Candesartan>100
Farglitazar0.01 ± 0.02