Cross-Species Differential Plasma Protein Binding of MBX-102/JNJ39659100: A Novel PPAR-𝛾 Agonist

Table 4

Differential activation of PPAR-γ by PPAR-γ agonists in the presence of 10% of human, rat, and mouse serum. Values are EC₅₀ (𝜇M) determined from 3 experiments and shown as the mean ± SD. FC is the ratio of EC₅₀s for human: rat or human: mouse (* = 𝑃<.05, ** = 𝑃<.01, *** = 𝑃<.001 by ANOVA with Tukey post hoc test).

PPAR agonist	Mean EC50 (𝜇M) ± SD			Fold Change in EC50
	Human	Rat	Mouse	Human:Rat	Human:Mouse
MBX-102 acid	260 ± 16.9	196 ± 18	169 ± 5.2	1.33^**	1.53^***
Rosiglitazone	2.0±0.1	5.2±0.3	4.5±0.3	0.39^***	0.45^***
Pioglitazone	8.3±0.4	11.4±1.2	9.7±1.4	0.73^NS	0.86^NS