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
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3 , with an IC 50 of 12 nM for human GSK-3β . SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)
In Vitro
SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ 25-35 -induced cell death in rat embryonic hippocampal neurons. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mice expressing P301L tau. SAR502250 (10-30 mg/kg; p.o. once daily for 7 weeks) improves the cognitive deficit in transgenic APP(SW)/Tau(VLW) mice after infusion of Aβ 25-35. SAR502250 (10-30 mg/kg; a single p.o.) significantly increases the percentage of lever-presses in the inter-response time (IRT) bin (49-96 s), with a significant augmentation of the percentage of reinforced responses. SAR502250 (30 mg/kg; i.p. once daily for 28 d) ameliorates chronic stress-induced degradation of the physical state of the mice coat. SAR502250 (10-60 mg/kg; a single p.o.) decreases hyperactivity produced by psychostimulantsin mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female P301L human tau transgenic mice (three-month-old; 32 g)Dosage: 1, 3, 10, 30, 100 mg/kg Administration: A single p.o. Result: Attenuated dose-dependently tau phosphorylation in the cortex and spinal cord, with ED 50 s of 12.5 and 11.5 mg/kg, respectively.
IC50& Target:hGSK-3β 12 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
SAR502250
生化机理
SAR502250 是一种强效、选择性、ATP 竞争性、口服活性和脑穿透性 GSK3 抑制剂，对人 GSK-3β 的 IC 50 为 12 nM。SAR502250 具有类似抗抑郁剂的活性。SAR502250 可用于阿尔茨海默病的研究。
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
CN1C(=O)C=C(N=C1N2CCO[C@H](C2)C3=CC=C(C=C3)F)C4=NC=NC=C4
PubChem CID
分子量
367.38
技术文档
高级数据
关联靶点（人）
GSK3B
Tclin
糖原合酶激酶-3β(Glycogen synthase kinase-3 beta)
(2 活性数据)
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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