BMS-779788 is a LXR partial agonist with IC 50 values of 68 nM for LXR α and 14 nM for LXR β .
In Vitro
The LXR selective partial agonist BMS-779788 is identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC 50 =1.2 μM, 55% efficacy). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BMS-779788 induces LXR target genes in blood in vivo with an EC 50 =610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 is 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B . In mice BMS-779788 displays peripheral induction of ABCA1 at 3 and 10 mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
