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Biological Activity:
A highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%; ref 1); potently induces luciferase reporter expression with an EC50 value of 16 nM (ref 2).
References:
B Flutt et al. Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR). J. Med. Chem. 2009, 52(4), 904–907. [online]
MJ Evans et al. A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia. Am. J. Physiol. Gastrointest. Liver Physiol. 2009, 296(3), G543-G552. [online]
HB Hartman et al. Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/− and apoE−/− mice. J. Lipid Res. 2009, 50(6), 1090-1100. [online]
S Zhang et al. Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis. J Hepatol. 2009, 51(2), 380-388. [online]
Chemical Name: Isopropyl 3-(3,4-difluorobenzoyl)-1,1-dimethyl-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate
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