计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
为什么选择此级别
提供 ≥98% 纯度，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
-20°C储存。超低温运输 。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
E1231 is an orally active activator of Sirtuin 1 ( SIRT1 ) ( EC 50 =0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (K D =9.61 μM) and deacetylated liver X receptor-alpha ( LXRα ), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases
In Vitro
E1231 (0.1-10 μM; 18 h) promotes cholesterol efflux and inhibits lipid accumulation in RAW 264.7 cells. E1231 (10 μM; 6 h) significantly increases deacetylation of Doxo-induced p53 in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
E1231 (40 mg/kg; po; once daily for 7 days) regulates cholesterol and lipid metabolism in Golden hamsters fed with HFD diet . E1231 (25, 50, and 100 mg/kg, in 0.5% CMC-Na; po; once daily for 12 weeks) reduces atherosclerosis development, without hepatotoxicity ornephrotoxicity in ApoE -/- mice fed with atherogenic diet . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: HFD-diet Golden hamsters (80-90 g) Dosage: 40 mg/kg Administration: PO; once daily for 7 days Result: Increased SIRT1 protein expression but not SIRT3, SIRT6, or SIRT7. And reduced liver and serum cholesterol in hamsters. Animal Model: Atherogenic diet ApoE -/- mice Dosage: 25, 50, and 100 mg/kg Administration: PO; once daily for 12 weeks Result: Modulated plaque composition, immunofluorescence staining. And reduced CD68 positive areas while increasing ABCA1 expression in the aortic sinus.
Form:Solid
IC50& Target:SIRT1 0.83 μM (EC 50 )
规格
规格或纯度
≥98%
英文名称
E1231
生化机理
E1231 是一种具有口服活性的 Sirtuin 1（SIRT1）激活剂（EC 50 =0.83 μM），可调节胆固醇和脂质代谢。E1231 能与 SIRT1（K D =9.61 μM）和去乙酰化的肝 X 受体-α（LXRα）相互作用，并能增加 ATP 结合盒信号传导。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
激活剂
纯度
≥98%
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=CC=C(O1)C2=NC3=CC=CC=C3C(=C2)C(=O)N4CCN(CC4)C(=O)C
PubChem CID
分子量
363.41
技术文档
高级数据
关联靶点（人）
GBA1
Tclin
Beta-glucocerebrosidase
(14647 活性数据)
GLP1R
Tclin
Glucagon-like peptide 1 receptor
(111429 活性数据)
HepG2
(196354 活性数据)
POLI
Tchem
DNA polymerase iota
(116820 活性数据)
BRCA1
Tchem
Breast cancer type 1 susceptibility protein
(15908 活性数据)
TDP1
Tchem
Tyrosyl-DNA phosphodiesterase 1
(345557 活性数据)
GMNN
Tbio
Geminin
(128009 活性数据)
ATAD5
Tbio
ATPase family AAA domain-containing protein 5
(122566 活性数据)
关联靶点（其它种属）
GCN5
Histone acetyltransferase GCN5 (89 活性数据)
Luciferin 4-monooxygenase (66902 活性数据)
Txnrd1
Thioredoxin reductase 1, cytoplasmic (45279 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 100 mg/mL (275.17 mM; Need ultrasonic)
分子量
363.400 g/mol
XLogP3
2.100
氢键供体数Hydrogen Bond Donor Count
0
氢键受体数Hydrogen Bond Acceptor Count
4
可旋转键计数Rotatable Bond Count
2
精确质量Exact Mass
363.158 Da
单同位素质量Monoisotopic Mass
363.158 Da
拓扑极表面积Topological Polar Surface Area
66.700 Ų
重原子数Heavy Atom Count
27
形式电荷Formal Charge
0
复杂度Complexity
561.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
0
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
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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