GSK-3β inhibitor 2  ≥98%

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包装规格:5mg 10mg 50mg 100mg in glass bottle
产品简介:一种有效,选择性和口服活性的GSK-3β抑制剂,IC50为1.1nM。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。
溶解性:溶于DMSO(5mg/mL超声)
储备液保存:-80°C, 2 years -20°C, 1 year
靶点:GSK-3β:1.1 nM (IC50)
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.
保存条件:-20℃
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