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编 号:F762648
分子式:C12H17N5O
分子量:247.3
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生物活性:
nSMase2-IN-1 is an orally active Neutral sphingomyelinase 2 (nSMase2) inhibitor with an IC50 value of 0.13 ± 0.06 μM. nSMase2-IN-1 is metabolically stable in liver microsomes and orally available with a favorable brain-to-plasma ratio. nSMase2-IN-1 can be used for nervous system disease research.

体内研究:
nSMase2-IN-1 (Compound 11j) (10 mg/kg, 口服灌胃, 30 min 和 2 h 后取样检测) 口服有效,在雄性Wistar 大鼠中具有脑渗透作用。Animal Model:Male Wistar rats (Pharmacokinetic assay)
Dosage:10 mg/kg
Administration:Oral gavage (p.o.)
Result:Absorbed quickly resulting in plasma concentration of more than 2 μM and had higher brain levels than plasma at 0.5 h.

体外研究:
nSMase2-IN-1 (Compound 11j) (5μM, 60 分钟) 在大鼠肝微粒体中表现出良好的代谢稳定性,1 小时后残留 95%。
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