计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
XL041 (BMS-852927) is an LXRβ -selective agonist.
In Vitro
XL041 (BMS-852927) is an LXRβ-selective agonist with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. XL041 is potent, with an EC 50 =9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
XL041 (BMS-852927), has a very favorable profile at efficacious doses in cynomolgus monkeys and mice. XL041 pre-treatment of C57BL/6J mice for 7 days results in potent, dose-dependent stimulation of cholesterol efflux in this system, reaching a maximum in the 3 mg/kg/day dose group of 70% above vehicle in the initial efflux rate. Similar results are obtained in LDLR knockout (KO) mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO mice. Importantly, the dose response for inhibition of atherosclerosis (0.1-3 mg/kg/day) is similar to the dose response for macrophage reverse cholesterol transport (RCT) stimulation (0.03-3 mg/kg/day), a major underlying mechanism through which LXR agonists affect the disease . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:LXRβ
规格
规格或纯度
10mM in DMSO
英文名称
XL041
生化机理
XL041 （BMS-852927）是一种 LXRβ 选择性激动剂。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)(C1=CN(C(=N1)C(C)(C)C2=C(C=CC=C2Cl)Cl)C3=C(C=C(C=C3)C4=CC(=C(C(=C4)S(=O)(=O)C)CO)F)F)O
关联CAS
PubChem CID
分子量
609.51
技术文档
高级数据
关联靶点（人）
NR1H2
Tchem
氧固醇受体 LXR-β(Oxysterols receptor LXR-beta)
(4 活性数据)
NR1H3
Tchem
氧固醇受体 LXR-alpha(Oxysterols receptor LXR-alpha)
(2 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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危险品化学品经营许可证（带存储）