BMS-779788,918348-67-1

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BMS-779788

CAS No. : 918348-67-1

MCE 国际站：BMS-779788

产品活性：BMS-779788是LXR的部分激动剂，其对LXRα和LXRβ的IC₅₀值分别为68和 14 μM。

研究领域：Metabolic Enzyme/Protease  |  Vitamin D Related/Nuclear Receptor

作用靶点：LXR

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 (EC₅₀=1.2 μM, 55% efficacy).

In Vivo: BMS-779788 induces LXR target genes in blood in vivo with an EC₅₀=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.

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