SR 1664

SR 1664

CAT N°: 11086
Price:

68.00 57.80

Apart from direct peroxisome proliferator-activated receptor ? (PPAR?) agonism, several PPAR? ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPAR? by cyclin-dependent kinase 5 (Cdk5) at serine 273.{25001} This effect requires binding to the PPAR? ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor ? (PPAR?) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPAR? receptor.{25002} It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.{25002}

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