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GSK2324 is a FXR agonist (EC50 = 50 nM, 102% efficacy). | [Uses]
GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively[1]. | [References]
[1] Jonathan Y Bass, et al. Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1206-13. DOI:10.1016/j.bmcl.2010.12.089 |
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