BMS-779788 (Synonyms: EXEL04286652; XL-652; BMS-788)
目录号: PL06807 纯度: ≥99%
CAS No. :918348-67-1
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中文名称
BMS-779788
中文别名
BMS-779788
英文名称
BMS-779788
英文别名
BMS-779788;NULL;BMS779788;BMS788;BMS-788;XL652;XL-652;2-{2-[2-(2-Chlorophenyl)propan-2-Yl]-1-[3'-(Methylsulfonyl)biphenyl-4-Yl]-1h-Imidazol-4-Yl}propan-2-Ol;2-(2-(2-(2-chlorophenyl)propan-2-yl)-1-(3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)-1H-imidazol-4-yl)propan-2-ol;4rak;FB7ZTJ8M8A;BCP20751;BDBM50034775;Q27456220;1H-Imidazole-4-methanol,2-[1-(2-chlorophenyl)-1-methylethyl]-a,a-dimethyl-1-[3'-(methylsulf
Cas No.
918348-67-1
分子式
C28H29ClN2O3S
分子量
509.06
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
BMS-779788 is a LXR partial agonist with IC 50 values of 68 nM for LXRα and 14 nM for LXRβ.
性状
Solid
IC50 & Target[1][2]
IC50: 68 nM (LXRα); 14 nM (LXRβ)
体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Kirchgessner TG, et al. Pharmacological characterization of a novel liver X receptor agonist with partial LXRα activity and a favorable window in nonhuman primates. J Pharmacol Exp Ther. 2015 Feb;352(2):305-14.
[2]. Kick E, et al. Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ. Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7.
溶解度数据
In Vitro: DMSO : 100 mg/mL (196.44 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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