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 |
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Moligand™ 级 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。
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
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。
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。
FKGK18 is a selective group VIA calcium-independent phospholipase A 2 (GVIA iPLA 2 ) inhibitor. FKGK18 is a fluoroketone (FK)-based compound with IC 50 s of 50 nM and 3 μM for iPLA 2 β and iPLA 2 γ. FKGK18 can be used for the research of beta-cell apoptosis and diabetes
In Vitro
FKGK18 (1 nM; 1 h) inhibits glucose-stimulated insulin secretion (GSIS) and prostaglandin E2 (PGE2) generation. FKGK18 (0.1-10 nM; 24 h) inhibits beta-cell apoptosis. FKGK18 (0.1-10 μM; 24 h) affects immune cells function and influences B-cell survival. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human pancreatic islets Concentration: 1 nM Incubation Time: 1 h Result: Inhibited GSIS from pancreatic islets, AA hydrolysis from beta-cells membranes and PGE2 generation. Penetrated islets and the beta-cells from islets. Apoptosis AnalysisCell Line: INS-1 OE cells Concentration: 0.1-10 nM Incubation Time: 24 h Result: Inhibited beta-cells apoptosis induced by ER-stress. Cell Viability AssayCell Line: CD4 + T-cell and B-cell from 8–12-week-old NOD female mice Concentration: 0.1-10 μM/L Incubation Time: 24 h Result: Decreased TNF-α generation, reduced viability of B cell and antibody production.
In Vivo
FKGK18 (20 mg/kg; i.p. three times per week from 10 days until euthanasia) reduces diabetes incidence. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 10-day-old female NOD miceDosage: 20 mg/kg Administration: Intraperitoneal injection; 20 mg/kg three times per week; from 10 days until euthanasia Result: Reduced diabetes incidence and maintained better glucose homeostasis.
Form:Solid
IC50& Target:IC50: 50 nM (iPLA2β), 3 μM (iPLA2γ)
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 苯类化合物 |
| 类(Class) | 萘 |
| 亚类(Subclass) | 暂无 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 萘 |
| 其他上位类(Alternative Parents) | α-卤代酮 有机氟化物 有机氧化物 碳氢化合物衍生物 烷基氟化物 |
| 分子骨架(Molecular Framework) | 芳香族同多环化合物 |
| 取代基(Substituents) | 氟化烷基 - 烷基溴化物 - α-卤代酮 - 芳香族同多环化合物 - 羰基 - 烃衍生物 - 酮 - 萘 - 有机氧化物 - 有机氧化合物 - 有机氟化物 - 有机卤化物 - 有机氧化合物 |
| 描述(Description) | 该化合物属于萘类有机化合物。这类化合物含有萘基团,即两个共熔的苯环结构。 |
| 外部描述符(External Descriptors) | 暂无 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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