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G3335 is a cell-permeable dipeptide that potently antagonizes PPARγ (Kd = 8.34 µM).1 It reversibly and competitively blocks activation of PPARγ by rosiglitazone (IC50 = 8-32 µM).1 G3335 is active in vivo, abolishing the protective effects of rosiglitazone in experimental spinal cord injury in rats.2 G3335 has also been used to evaluate the role of PPARγ in neurotoxicity studies.3,4
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1. The dipeptide H-
2. Rosiglitazone enhances the proliferation of neural progenitor cells and inhibits inflammation response after spinal cord injury. Neurosci. Lett. 503, 191-195 (2011).
3. PPAR-
4. Oxaliplatin neurotoxicity involves peroxisome alterations. PPARγ agonism as preventive pharmacological approach. PLoS One 9(7), 1-15 (2014).