• 產(chǎn)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(nèi)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(xiàn)：
  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(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *