T0070907

T0070907

CAT N°: 10026
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From 20.00 17.00

The peroxisome proliferator-activated receptor-? (PPAR?) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPAR? receptor agonists with antidiabetic actions in vivo.{7575,8930} There are many PPAR? agonists, including 15-deoxy-?12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8953,8224} However, only a few antagonists have been reported.{8241} T0070907 is a potent and selective antagonist of the human PPAR? with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPAR?, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPAR?/RXR heterodimer.{10311}

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