GW0742
PPAR β/δ receptor Agonist compound From Wikipedia, the free encyclopedia
GW0742 (also known as GW610742 and fitorine) is a PPARδ/β agonist[2][3][4] that has been investigated for drug use by GlaxoSmithKline.[5]
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| Formula | C21H17F4NO3S2 |
| Molar mass | 471.48 g·mol−1 |
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Pharmacology
Pharmacodynamics
It is mixed PPAR-B agonist antagonist depending on its dosage.[6] It has weak activity on multiple nuclear receptors as well. It is antagonistic at androgen receptors and VDR.[6][7] In silico modelling suggest that it has effects on thyroid hormone receptors.[8]
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.[7] Other novel analogues which are more potent than GWO742 with reduced toxicity have been developed as well.[9]
Research
GW0742 has been shown to ameliorate experimentally induced pancreatitis in mice.[10] Additionally, it prevents hypertension in diet induced obese mice,[11] has been investigated as potential antidiabetic drug,[12] and has anti-inflammatory effects.[13][14][11]
See also
References
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