GW0742 is a highly selective PPARδ agonist. EC50 = 1 nM vs 1 μM and 2 μM for PPARα and PPARγ, respectively.
특징 및 장점
This compound is featured on the Nuclear Receptors (PPARs) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
법적 정보
Sold for research purposes under agreement from GlaxoSmithKline
The Journal of biological chemistry, 292(3), 884-897 (2016-12-04)
Peroxisome proliferator-activated receptor δ (PPARδ) regulates many genes involved in lipid metabolism. Hepatic lysophosphatidylcholine acyltransferase 3 (LPCAT3) has critical functions in triglycerides transport and endoplasmic reticulum stress response due to its unique ability to catalyze the incorporation of polyunsaturated fatty
Osteoarthritis (OA) is an inflammatory joint disease characterized by degeneration of articular cartilage within synovial joints. An estimated 27 million Americans suffer from OA, and the population is expected to reach 67 million in the United States by 2030. Thus
Diabetic retinopathy (DR) is triggered by retinal cell damage stimulated by the diabetic milieu, including increased levels of intraocular free fatty acids. Free fatty acids may serve as an initiator of inflammatory cytokine release from Müller cells, and the resulting
Pulmonary alveolar septa are thought to contain at least two types of fibroblasts that are termed myofibroblasts and lipofibroblasts based on their morphological characteristics. Lipofibroblasts possess cytoplasmic lipid inclusions (lipid bodies or droplets) and are involved in several important functions
Clinical science (London, England : 1979), 130(20), 1823-1836 (2016-07-15)
PPARβ/δ activation protects against endothelial dysfunction in diabetic models. Elevated glucose is known to impair cAMP-induced relaxation and Kv channel function in coronary arteries (CA). Herein, we aimed to analyse the possible protective effects of the PPARβ/δ agonist GW0742 on