BMS-779788 (C09-1112-976)

BMS-779788 is a LXR partial agonist with IC 50 values of 68 nM for LXR α and 14 nM for LXR β .In VitroThe 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 VivoBMS-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.Form:SolidIC50& Target:IC50: 68 nM (LXR α ),14 nM (LXR β ). Specification: 0.99 Molecular Formula: C28H29ClN2O3S Molecular Weight: 509.06 PubChem CID: 59251511 Isomeric SMILES: CC(C)(C1=CC=CC=C1Cl)C2=NC(=CN2C3=CC=C(C=C3)C4=CC(=CC=C4)S(=O)(=O)C)C(C)(C)O