Rosiglitazone 122320-73-4

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Molecular Weight:

357.43 Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively.






Biological Activity


Rosiglitazone markedly increase phosphorylation of threonine 172 within
the α subunit of AMPK, with increased AMP:ATP ratio. Rosiglitazone has
been reported to decrease cholesterol synthesis in a number of cell
lines in a peroxisome proliferator-activated receptor γ-independent
manner. Rosiglitazone activates both α1- and α2-containing AMPK
complexes, and this leads to a marked increase in the phosphorylation of
acetyl-CoA carboxylase.


Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro. Rosiglitazone increases adiponectin secretion from omental cells up to
2.3-fold higher, whereas secretion from subcutaneous adipose cells is
unaffected. Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes.


Rosiglitazone administration results in significant bone loss, including
a decrease in bone volume, trabecular width, and trabecular number and
an increase in trabecular spacing. Rosiglitazone also leads to a
decrease in bone formation rate, with a simultaneous increase in fat
content in the bone marrow.


Rosiglitazone decreases the expression of
the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen,
whereas the expression of the adipocyte-specific fatty acid binding
protein aP2 is increased. Rosiglitazone upregulates gene
transcripts encoding mitochondrial Proteins in white adipocytes from
ob/ob mice accompanied by an increase in mitochondrial mass and changes
in mitochondrial structure.

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