ASP-2535 是一种高效、有口服活性、选择性的，脑渗透性和中心活性的 GlyT1 抑制剂。ASP-2535 能改善精神分裂症和阿尔茨海默病动物模型的认知障碍。
货号:ajcx15560
CAS:374886-51-8
分子式:C22H18N6O
分子量：382.42
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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 Alzheimer's disease[1].

ASP2535 potently inhibits rat GlyT1 (IC50=92 nM) with 50-fold selectivity over rat glycine transporter-2 (GlyT2) in vitro[1].

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[1].ASP2535 (1-3 mg/kg, p.o.) also improves the PCP-induced deficit in prepulse inhibition in rats[1]. Animal Model: 5-week-old male ddY mice[1]

[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 Alzheimer's disease. Eur J Pharmacol. 2012 Jun 15;685(1-3):59-69.