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1702428-31-6

中文名稱 GSK-3 β inhibitor 2
英文名稱 GSK-3 β inhibitor 2
CAS 1702428-31-6
分子式 C14H14N4O3S
分子量 318.35
MOL 文件 1702428-31-6.mol
1702428-31-6 結(jié)構(gòu)式 1702428-31-6 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11471
GSK-3Β 抑制劑 2
2-(2-(環(huán)丙烷甲酰胺基)吡啶-4-基)-4-甲氧基噻唑-5-甲酰胺
英文別名
GSK-3β inhibitor 2
GSK-3 β inhibitor 2

物理化學(xué)性質(zhì)

密度1.475±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)13.08±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
GSK-3 β inhibitor 2價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-130795GSK-3 β inhibitor 2
GSK-3β inhibitor 2
1702428-31-65mg1750元
2024/11/08HY-130795GSK-3 β inhibitor 2
GSK-3β inhibitor 2
1702428-31-610mg2800元
2024/11/08HY-130795GSK-3 β inhibitor 2
GSK-3β inhibitor 2
1702428-31-610mM * 1mLin DMSO3850元

常見問題列表

生物活性
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 (IC 50 )

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.

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