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INT 131 is a potent and selective PPARγ partial agonist (EC50 = 4 nM; Ki = 3.7 nM). It has a 20-fold higher affinity for PPARγ compared with that of Rosiglitazone (Cat. No. 5325). INT 131 improves glucose tolerance in a rodent model of diabetes without inducing hemodynamic and cardiovascular effects. Antidiabetic agent.
|Storage||Store at -20°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|
The following data is based on the product molecular weight 514.21. 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|
|0.05 mM||38.89 mL||194.47 mL||388.95 mL|
|0.25 mM||7.78 mL||38.89 mL||77.79 mL|
|0.5 mM||3.89 mL||19.45 mL||38.89 mL|
|2.5 mM||0.78 mL||3.89 mL||7.78 mL|
References are publications that support the biological activity of the product.
Frkic et al (2017) Structure-activity relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) analogs for PPARγ-targeted antidiabetics. J.Med.Chem. 60 4584 PMID: 28485590
Motani et al (2009) INT131: a selective modulator of PPARγ. J.Mol.Biol. 386 1301 PMID: 19452630
If you know of a relevant reference for INT 131, please let us know.
Keywords: INT 131, INT 131 supplier, INT131, PPARγ, PPARgamma, partial, agonists, antidiabetics, agent, Peroxisome, Proliferator-activating, Receptors, in, vivo, diabetes, 7423, Tocris Bioscience
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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.