货号	规格	价格	上海	北京	珠海	重庆	武汉
S20616-1mg	≥98%	￥240.00 S20616-1mg ￥240.00 3-5天	0 货期：3-5天	-	-	-	-
S20616-5mg	≥98%	￥350.00 S20616-5mg ￥350.00 3-5天	0 货期：3-5天	-	-	-	-
S20616-10mg	≥98%	￥465.00 S20616-10mg ￥465.00 3-5天	0 货期：3-5天	-	-	-	-
S20616-25mg	≥98%	￥720.00 S20616-25mg ￥720.00 3-5天	0 货期：3-5天	-	-	-	-
S20616-50mg	≥98%	￥1370.00 S20616-50mg ￥1370.00 3-5天	0 货期：3-5天	-	-	-	-
S20616-100mg	≥98%	￥2500.00 S20616-100mg ￥2500.00 3-5天	0 货期：3-5天	-	-	-	-
S20616-1g	≥98%	￥21000.00 S20616-1g ￥21000.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

GSK-3β inhibitor 2 (Compound 3) 是一种有效，选择性和口服活性的 GSK-3β 抑制剂，IC50 为 1.1 nM。GSK-3β inhibitor 2 可以穿越血脑屏障。GSK-3β inhibitor 2 有用于阿尔茨海默氏病的潜力。

靶点：

GSK-3β 1.1 nM (IC50);GSK-3

体外研究：

The pyridine carboxamide of GSK-3β inhibitor 2 (Compound 3) makes hydrogen bonds with the hinge V135 backbone amide, and the carbonyl oxygen of the thiazolyl primary amide formed a critical hydrogen bond with K85. The quality of the electron density for the methyl group of the methoxy moiety in GSK-3β inhibitor 2 does not allow its unambiguous placement in the model, but a small molecule crystal structure of GSK-3β inhibitor 2 determined by single crystal X-ray diffraction method confirmed the intramolecular hydrogen bonding between the methoxy -O- and the amide N-H in GSK-3β inhibitor 2.

体内研究：

The elevation of hyperphosphorylated Tau (pTau) is mimicked in LaFerla 3xTg-C57BL6 mice, and accordingly, these mice are used as an in vivo model of Alzheimer’s disease. GSK-3β inhibitor 2 (Compound 3) shows a significant reduction in pTau396 when administered orally at 30 mg/kg as a nanosuspension to LaFerla 3xTg-C57BL6 male mice. GSK-3β inhibitor 2 shows only modest brain exposure (B/P = 0.26) as determined as a single time point.

参考文献：

1.Sivaprakasam P, et al. Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core. Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.141 ml	15.706 ml	31.412 ml
5 mM	0.628 ml	3.141 ml	6.282 ml
10 mM	0.314 ml	1.571 ml	3.141 ml
50 mM	0.063 ml	0.314 ml	0.628 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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