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产品目录

LXR激动剂(BMS-779788)图片
产品货号:
M05385
中文名称:
LXR激动剂(BMS-779788)
英文名称:
BMS-779788
产品规格:
1mL(10mM)|5mg|10mg|25mg|50mg|100mg
发货周期:
1~3天
产品价格:
询价
BMS-779788是LXR的部分激动剂,其对LXRα和LXRβ的IC50值分别为68和14μM。
注:本品仅可用于科研实验,严禁用于临床医疗及其他用途!


CAS号:918348-67-1
别名:EXEL04286652;XL-652;BMS-788
纯度:98.0%
分子式:C28H29ClN2O3S
分子量:509.06
结构式:
    BMS-779788结构式
保存:-20℃,有效期2年,溶入溶剂后-20℃请尽量在一个月内使用。


体外研究The LXR selective partial agonist BMS-779788 is identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2μM,55% efficacy).
体内研究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.



Animal Administration
Monkeys:Male cynomolgus monkeys are used in the study.For a single-dose pharmacokinetic (PK)-pharmacodynamic (PD) study,2 animals each are treated either with vehicle [0.5% carboxymethyl cellulose and 2% Tween 80 in purified water) or 1mg/kg BMS-779788.For the 7 day PD study,18 animals are randomized into 6 treatment groups (N=3/group;3-6 kg) and received the following treatments at 7 AM daily for 7 days by oral gavage:vehicle,10mg/kg per day T0901317 and 0.3,1,3,or 10mg/kg per day BMS-779788
相关搜索:LXR激动剂(BMS-779788)EXEL04286652XL-652BMS-788918348-67-1
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