1702428-31-6
基本信息
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
GSK-3 β inhibitor 2
物理化學(xué)性質(zhì)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-130795 | GSK-3 β inhibitor 2 GSK-3β inhibitor 2 | 1702428-31-6 | 5mg | 1750元 |
2024/11/08 | HY-130795 | GSK-3 β inhibitor 2 GSK-3β inhibitor 2 | 1702428-31-6 | 10mg | 2800元 |
2024/11/08 | HY-130795 | GSK-3 β inhibitor 2 GSK-3β inhibitor 2 | 1702428-31-6 | 10mM * 1mLin DMSO | 3850元 |
常見問題列表
GSK-3β 1.1 nM (IC 50 ) |
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.
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.