ASP 2535;ASP2535;6627LI8F9K;4-[3-(1-Methylethyl)-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole;4-(3-(1-Methylethyl)-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl)-2,1,3-benzoxadiazole;2,1,3-Benzoxadiazole, 4-(3-(1-methylethyl)-5-(6-phenyl-3-pyridinyl)-4H-1,2,4-triazol-4-yl)-
ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimers disease.
性状
Solid
IC50 & Target[1][2]
GlyT1
体外研究(In Vitro)
ASP2535 potently inhibits rat GlyT1 (IC50=92 nM) with 50-fold selectivity over rat glycine transporter-2 (GlyT2) in vitro. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ASP2535 (0.3-3 mg/kg; p.o) attenuates working memory deficit in MK-801-treated mice and visual learning deficit in neonatally phencyclidine (PCP)-treated mice.
ASP2535 (1-3 mg/kg, p.o.) also improves the PCP-induced deficit in prepulse inhibition in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Harada K, et al. A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimers dis