GW0742
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GW0742 (also known as GW610742) is a PPARδ/β agonist that is investigated for drug use by GlaxoSmithKline.


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 has been developed. One of the compound, which has 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 has been developed as well.


Research

GW0742 has been shown to ameliorate experimentally induced pancreatitis in mice. It also prevents hypertension in diet induced obese mice. and is investigated as potential antidiabetic drug as well. It is anti-inflammatory agent as well.


See also

*
GW501516 GW501516 (also known as GW-501,516, GW1516, GSK-516, Cardarine, and on the black market as Endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It entere ...
* Elafibranor *
Peroxisome proliferator-activated receptor In the field of molecular biology, the peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes. PPARs play essential roles in the regu ...


References

PPAR agonists GSK plc brands Experimental drugs Trifluoromethyl compounds Thiazoles Fluoroarenes Thioethers {{pharma-stub