Peer-reviewed veterinary case report
Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR).
- Journal:
- Journal of medicinal chemistry
- Year:
- 2009
- Authors:
- Flatt, Brenton et al.
- Affiliation:
- Department of Medicinal Chemistry · United States
- Species:
- rodent
Abstract
Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist (EC(50) = 4 nM, Eff = 149%). Oral administration of 6m to LDLR(-/-) mice results in lowering of cholesterol and triglycerides. Chronic administration in an atherosclerosis model results in significant reduction in aortic arch lesions.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/19159286/