GW0742 (also known as GW610742 and fitorine) is a PPARδ/β

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

that has been investigated for drug use by

GlaxoSmithKline GSK plc (an acronym from its former name GlaxoSmithKline plc) is a British Multinational corporation, multinational Pharmaceutics, pharmaceutical and biotechnology company with headquarters in London. It was established in 2000 by a Mergers an ...

Pharmacology

Pharmacodynamics

It is mixed PPAR-B agonist antagonist depending on its dosage. It has weak activity on multiple nuclear receptors as well. It is antagonistic at androgen receptors and VDR. In silico modelling suggest that it has effects on thyroid hormone receptors.

Chemistry

Derivatives

Multiple derivatives of GW0742 core structure have been developed. One of the compounds has the thiazole ring replaced with an oxazole ring inhibited VDR-meditated transcription with IC₅₀ of 660 nM. Other novel analogues which are more potent than GWO742 with reduced toxicity have been developed as well.

Research

GW0742 has been shown to ameliorate experimentally induced pancreatitis in mice. Additionally, it prevents hypertension in diet induced obese mice, has been investigated as potential antidiabetic drug, and has anti-inflammatory effects.

References