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Potent, selective non-thiazolidinedione PPARγ partial agonist (EC50 = 57 nM); produces ~25% maximum efficacy. Antagonizes full agonist activity by ~60% (IC50 ~ 285 nM). Displays no activity at PPARα or PPARδ receptors. Produces altered receptor conformation, and regulates adipocyte development and gene expression, in a differential manner to full PPARγ agonists. Modulates metabolism and insulin sensitivity without causing cardiac hypertrophy in mice in vivo.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 428.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.33 mL||11.67 mL||23.35 mL|
|5 mM||0.47 mL||2.33 mL||4.67 mL|
|10 mM||0.23 mL||1.17 mL||2.33 mL|
|50 mM||0.05 mL||0.23 mL||0.47 mL|
References are publications that support the biological activity of the product.
Berger et al (2003) Distinct properties and advantages of a novel peroxisome proliferator-activated protein γ selective modulator. Mol.Endocrinol. 17 662 PMID: 12554792
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Keywords: nTZDpa, nTZDpa supplier, Potent, selective, PPARγ, PPARgamma, partial, agonists, Peroxisome, Proliferator-activating, Receptors, 2150, Tocris Bioscience
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Literature in this Area
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.