SD-6

SD-6 is an orally active inhibitor of hAChE and hBChE with IC50 values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease[1].

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

hAChE:0.907 μM (IC50)

hBCHE:1.579 μM (IC50)

SD-6 (5-80 µM；24 h) 在 SH-SY5Y 细胞中具有神经保护作用[1]。 Cell Viability Assay[1] Cell Line: SH-SY5Y cells. Concentration: 5, 10, 20, 40 or 80 µM. Incubation Time: 24 h. Result: Exhibited toxicity to differentiated SH-SY5Y cell lines and has a protective effect on undifferentiated SH-SY5Y cell lines.

SD-6 (100、300 和 500 mg/kg；口服；单剂量) 对未怀孕的雌性 Wistar 大鼠没有毒性作用[1]。 SD-6 (2.5、5 和 10 mg/kg；口服；一天 3 次，持续 7 天) 改善了东莨菪碱 (HY-N0296) 诱导的雄性 Wistar 大鼠认知和记忆缺陷[1]。 SD-6 (2.5、5 和 10 mg/kg；口服；单剂量) 显著改善了大鼠中东莨菪碱诱导的异常，促进生化指标正常化[1]。 Animal Model: 10–11 weeks nonpregnant female Wistar rats (220–280 g)[1]. Dosage: 100, 300 and 500 mg/kg. Administration: Oral gavage; single dose. Result: Showed safety and tolerability. Animal Model: 10–11 weeks male Wistar rats (220–280 g)[1]. Dosage: 2.5、5、10 mg/kg. Administration: Oral gavage; 3 times a day for 7 days or single dose. Result: Had the function of repairing cognitive and memory deficits. Reduced the level of AChE and malonaldehyde (MDA), increased the level of acetylcholine, superoxide dismutase (SOD), glutathione (GSH) and catalase.

[1]. Waiker DK, et al. Development and Evaluation of Some Molecular Hybrids of N-(1-Benzylpiperidin-4-yl)-2-((5-phenyl-1,3,4-oxadiazol-2-yl)thio) as Multifunctional Agents to Combat Alzheimer's Disease. ACS Omega. 2023 Mar 2;8(10):9394-9414.