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PPAR 激动剂
Rosiglitazone (BRL-49653)是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。
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PPAR alpha/gamma agonist
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively.
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PPARα/γ dual agonist
Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
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PPAR-α antagonist
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively.
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PPARα antagonist
GW 6471 is a potent PPARα antagonist.
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dual α/γ PPAR activator
Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
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PPAR agonist
Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ).
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PPARα/PPARγ dual agonist
LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively.
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