Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 4'-[[2,3-dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid
Purity: ≥98%
Formula Markup: C33H29N3O5
Formula Weight: 547.6
CAS Number: 1338259-05-4
Notes: Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.{25001} This effect requires binding to the PPARγ 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 γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ 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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