CAS 857290-04-1: N-(6-amino-2-pyridyl)-4-(4-cyanophenyl)benzenesulfonamide

PF-915275 inhibits 11βHSD1 in humans (Ki=2.3 nM, EC50=15 nM) and affects cortisone-cortisol conversion in hepatocytes.

PF 915275 is a novel, orally active drug for the treatment of type 2 diabetes. It is an inhibitor of glucocorticoid receptor activity and has shown promising results in animal models for type 2 diabetes treatment. PF 915275 also has a potential role in treating metabolic disorders such as obesity, glucose intolerance, and hyperlipidemia. This drug is a potent inhibitor of the transcriptional activity of the glucocorticoid receptor, which leads to decreased cortisol levels in blood cells. The mechanism of action of PF 915275 involves the inhibition of phosphorylation by p-nitrophenyl phosphate (PNPP) on the glucocorticoid receptor and subsequent reduction in cAMP production. This results in decreased PGE2 levels and increased insulin secretion by pancreatic β-cells. PF 915275 binds to thyroid hormone receptors with high affinity and may have therapeutic implications for thyroid diseases such as Graves’ disease or Hashimoto’s thyroiditis.

PF-915275