RGNCY-0077 (1a PPARϒ agonist PPARδ anatgonist)

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Compound 1a significantly increases adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) which is associated with improved insulin sensitivity.  The adiponectin-promoting activity of 1a significantly correlates with its binding activity to both peroxisome proliferator activated receptor (PPAR) ϒ and PPARδ.  It is both a partial PPARϒ agonist and PPARδ anatgonist.  In the diabetic mouse (STZ induced) model, orally administered 1a significantly decreases glucose and triglyceride serum levels, supporting its anti-diabetic potential.  

SMILE: IC1=CC=CC(CCC2=NC=NC3=C2N=CN3[C@@H]4O[C@H](C(NC)=O)[C@H](O)[C@@H]4O)=C1 

Systematic Name:  (2S,3R,4S,5R)-3,4-dihydroxy-5-(6-(3-iodophenethyl)-9H-purin-9-yl)-N-methyltetrahydrofuran-2-carboxamide 

Molecular Weight: 509.30

Formula:  C19H20IN5O4

PMID:  28799755