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SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2].
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2].

| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 4,820 | 8-10周 | |
| 25 mg | ¥ 13,900 | 8-10周 | |
| 50 mg | ¥ 18,300 | 8-10周 | |
| 100 mg | ¥ 23,500 | 8-10周 | |
| 1 mL x 10 mM (in DMSO) | ¥ 5,290 | 8-10周 |
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| 产品描述 | SAR502250 is a potent, selective, ATP-competitive, orally active, and brain-penetrant GSK3 inhibitor with a human GSK-3β IC50 value of 12 nM. It exhibits antidepressant-like activity and is being researched for potential application in Alzheimer’s disease (AD) treatment. |
| 靶点活性 | GSK-3β (human):12 nM (IC50) |
| 体外活性 | SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2]. |
| 体内活性 | SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mice expressing P301L tau[2].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 Aβ25-35[2].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[2].SAR502250 (30 mg/kg; i.p. once daily for 28 d) ameliorates chronic stress-induced degradation of the physical state of the mice coat[2].SAR502250 (10-60 mg/kg; a single p.o.) decreases hyperactivity produced by psychostimulantsin mice[2]. |
| 分子量 | 367.38 |
| 分子式 | C19H18FN5O2 |
| CAS No. | 503860-57-9 |
| Smiles | Cn1c(nc(cc1=O)-c1ccncn1)N1CCO[C@H](C1)c1ccc(F)cc1 |
| 密度 | 1.38 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 100 mg/mL (272.2 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (8.98 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。 | ||||||||||||||||||||||||||||||||||||
对于不同动物的给药剂量换算,您也可以参考 更多