| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H17F4NO3S2 |
| Molecular Weight | 471.488 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(CSC2=CC(C)=C(OCC(O)=O)C=C2)SC(=N1)C3=CC=C(C(F)=C3)C(F)(F)F
InChI
InChIKey=HWVNEWGKWRGSRK-UHFFFAOYSA-N
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)
GW0742, also known as GW610742, is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. GW0742 treatment has a prominent anti-inflammatory effect in 5XFAD mice and suggests that PPARδ agonists may have therapeutic utility in treating AD. GW0742 has the ability to improve glucose homeostasis in diabetic rats through activation of PPAR-δ. Therefore, PPAR-δ is a good target for the development of antidiabetic drugs in the future.
CNS Activity
Originator
Approval Year
PubMed
Sample Use Guides
Mice: GW0742 (30 mg/kg) significantly decreases protein and mRNA levels of the pro-inflammatory cytokines IL-6, IL-1beta and TNFalpha in bronchial alveolar lavage fluid of mice.
Route of Administration:
Oral
GW0742 (0.2 uM and 1 uM) treatment results in significant increases in reporter activity of PPARβ/δ in N/TERT-1 keratinocytes. GW0742 (1 uM) results in significant inhibition in the average number of N/TERT-1 keratinocytes. GW0742 (1 uM) results in an increase in the number of cells in the G1 phase and a decrease in the number of cells in the S phase.
ACTIVE MOIETY
