| 產品描述： | GSK-3β inhibitor 2 (Compound 3) 是一種有效，選擇性和口服活性的 GSK-3β 抑制劑，IC50 為 1.1 nM。GSK-3β inhibitor 2 可以穿越血腦屏障。GSK-3β inhibitor 2 有用于阿爾茨海默氏病的潛力。 |
| 靶點： |
GSK-3β 1.1 nM (IC50);GSK-3 |
| 體外研究： |
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. |
| 體內研究： |
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. |
| 參考文獻： |
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. |
| 保存條件： |
-20°C |
| 配置溶液濃度參考： |
|
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： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京