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Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR)

Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR)

Brenton Flatt, Richard Martin, Tie-Lin Wang, Paige Mahaney, Brett Murphy, Xiao-Hui Gu, Paul Foster, Jiali Li, Parinaz Pircher, Mary Petrowski, Ira Schulman, Stefan Westin, Jay Wrobel, Grace Yan, Eric Bischoff, etc.

J Med Chem. 2009 Feb 26;52(4):904-7.

PMID: 19159286

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP629664819	WAY-362450		629664-81-9	Price

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