Identification of a subtype selective human PPARα agonist through parallel-array synthesis
Using solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids was synthesized. GW7647 (3) was identified as a potent, selective human PPARα agonist.
References (8)
- et al.
Chem. Biol.
(1997) - et al.
Prog. Lipid Res.
(1993) - et al.
J. Med. Chem.
(2000) - et al.
Nature
(1990)
There are more references available in the full text version of this article.
Cited by (164)
Therapeutic targets, novel drugs, and delivery systems for diabetes associated NAFLD and liver fibrosis
2021, Advanced Drug Delivery ReviewsThe transcription factors CREBH, PPARa, and FOXO1 as critical hepatic mediators of diet-induced metabolic dysregulation
2021, Journal of Nutritional BiochemistryDiscovery of novel modulators for the PPARα (peroxisome proliferator activated receptor α): Potential therapies for nonalcoholic fatty liver disease
2021, Bioorganic and Medicinal ChemistryThe ventral pallidum as a critical region for fatty acid amide hydrolase inhibition of nausea-induced conditioned gaping in male Sprague-Dawley rats
2019, NeuropharmacologyCitation Excerpt :This finding may be a reflection of the selectivity of GW7647. GW7647 is ∼200-fold selective for murine PPARα (EC50 = 0.001 μM for PPARα; EC50 = 1.3 μM for PPARγ; EC50 = 2.91 μM for PPARδ; Brown et al., 2001). The intra-VP anti-nausea effect of GW7647 is consistent with previous data from our group showing that systemic GW7647 (3 mg/kg, i.p.) reduced LiCl-induced gaping, without producing conditioned gaping on its own (Rock et al., 2017).
Copyright © 2001 Elsevier Science Ltd. All rights reserved.