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]

ATC code
  • None
Legal status
  • Investigational
CAS Number
PubChem CID
Quick facts Clinical data, ATC code ...
GW0742
Clinical data
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
  • [4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methyl phenoxy]-acetic acid[1]
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H17F4NO3S2
Molar mass471.48 g·mol−1
3D model (JSmol)
  • FC(F)(F)c3c(F)cc(c1nc(c(s1)CSc2cc(c(OCC(=O)O)cc2)C)C)cc3
  • InChI=1S/C21H17F4NO3S2/c1-11-7-14(4-6-17(11)29-9-19(27)28)30-10-18-12(2)26-20(31-18)13-3-5-15(16(22)8-13)21(23,24)25/h3-8H,9-10H2,1-2H3,(H,27,28)
  • Key:HWVNEWGKWRGSRK-UHFFFAOYSA-N
Close

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

Related Articles

Wikiwand AI