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
提供 ≥99% 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
2-8°C储存,干燥。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
SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA 2 inhibitor with an IC 50 of 0.06 nM
In Vitro
SB-435495 inhibits CYP450 3A4 with an IC 50 of 10 μM and the black membrane permeability is 0.017 cm/h. SB-435495 (5 μM; 24 h) significantly inhibits the expression of Lp-PLA 2 protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs. SB-435495 (5 μM; 24-72 h) significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: oxLDL-exposed human umbilical vein endothelial cells Concentration: 5 μM Incubation Time: 24 h Result: The expression of Lp-PLA 2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172). Cell Viability AssayCell Line: oxLDL-exposed human umbilical vein endothelial cells Concentration: 5 μM Incubation Time: 24, 48 and 72 h Result: Significantly increased cell viability.
In Vivo
SB-435495 (10 mg/kg; p.o.; once) inhibits plasma Lp-PLA 2 in the WHHL rabbit . SB-435495 (10 mg/kg; i.p.; daily for 28 days) effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin -diabetic Brown Norway rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Lp-PLA2 0.06 nM (IC 50 )
规格
规格或纯度
≥99%
英文名称
SB-435495
生化机理
SB-435495 是一种强效、选择性、可逆、非共价和口服活性 Lp-PLA 2 抑制剂，其 IC 50 为 0.06 nM。
储存条件
2-8°C储存,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C=C(C(=O)N=C3SCC4=CC=C(C=C4)F)CC5=CN(N=C5)C
Isomeric SMILES
CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C=C(C(=O)N=C3SCC4=CC=C(C=C4)F)CC5=CN(N=C5)C
PubChem CID
分子量
720.82
技术文档
高级数据
关联靶点（人）
PLA2G7
Tchem
血小板活化因子乙酰水解酶(Platelet-activating factor acetylhydrolase)
(3 活性数据)
PLA2G7
Tchem
LDL-associated phospholipase A2
(1338 活性数据)
CYP2D6
Tclin
Cytochrome P450 2D6
(33882 活性数据)
CYP1A2
Tchem
Cytochrome P450 1A2
(26471 活性数据)
CYP2C9
Tchem
Cytochrome P450 2C9
(32119 活性数据)
CYP2C19
Tchem
Cytochrome P450 2C19
(29246 活性数据)
CYP3A4
Tclin
Cytochrome P450 3A4
(53859 活性数据)
Homo sapiens
(32628 活性数据)
关联靶点（其它种属）
Canis familiaris (36305 活性数据)
Rattus norvegicus (775804 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 (138.73 mM; Need ultrasonic)
分子量
720.800 g/mol
XLogP3
6.500
氢键供体数Hydrogen Bond Donor Count
0
氢键受体数Hydrogen Bond Acceptor Count
9
可旋转键计数Rotatable Bond Count
15
精确质量Exact Mass
720.287 Da
单同位素质量Monoisotopic Mass
720.287 Da
拓扑极表面积Topological Polar Surface Area
99.300 Ų
重原子数Heavy Atom Count
51
形式电荷Formal Charge
0
复杂度Complexity
1190.000
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
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）