Timcodar (VX-853) Is a Non-FKBP12 Binding Macrolide Derivative That Inhibits PPARγ and Suppresses Adipogenesis

Figure 3

Timcodar increases glucocorticoid responsiveness by increasing the GRα to GRβ ratio. Measurement of GRα and GRβ mRNA was performed by real-time PCR analysis of differentiated 3T3-L1 adipocytes treated with vehicle (Ctrl), 1 μM FK506 (FK), 1 μM timcodar (VX), and 1 μM rapamycin (Rap). (a) GRα, (b) GRβ, and (c) the ratio of GRα/GRβ. ; (versus control); (timcodar versus rapamycin treatment) (±S.E.; ). (d) mRNA of glucocorticoid responsive genes PDK4, GILZ, and p21. (versus control); (timcodar versus rapamycin treatment) (±S.E.; ).

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