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ASP2535 Sale

目录号 : GC38888

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。

ASP2535 Chemical Structure

Cas No.:374886-51-8

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5mg
¥6,390.00
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10mg
¥10,800.00
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100mg 待询 待询

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产品描述

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.

Chemical Properties

Cas No. 374886-51-8 SDF
Canonical SMILES CC(C1=NN=C(C2=CC=C(C3=CC=CC=C3)N=C2)N1C4=CC=CC5=NON=C54)C
分子式 C22H18N6O 分子量 382.42
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.6149 mL 13.0746 mL 26.1493 mL
5 mM 0.523 mL 2.6149 mL 5.2299 mL
10 mM 0.2615 mL 1.3075 mL 2.6149 mL
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Research Update

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.PMID:22542656DOI:10.1016/j.ejphar.2012.04.013

Hypofunction of brain N-methyl-d-aspartate (NMDA) receptors has been implicated in psychiatric disorders such as schizophrenia and Alzheimer's disease. Inhibition of glycine transporter-1 (GlyT1) is expected to increase glycine, a co-agonist of the NMDA receptor and, consequently, to facilitate NMDA receptor function. We have identified ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole) as a novel GlyT1 inhibitor, and here describe our in vitro and in vivo characterization of this compound. ASP2535 potently inhibited rat GlyT1 (IC(50)=92 nM) with 50-fold selectivity over rat glycine transporter-2 (GlyT2). It showed minimal affinity for many other receptors except for μ-opioid receptors (IC(50)=1.83 μM). Oral administration of ASP2535 dose-dependently inhibited ex vivo [(3)H]-glycine uptake in mouse cortical homogenate, suggesting good brain permeability. This profile was confirmed by pharmacokinetic analysis. We then evaluated the effect of ASP2535 on animal models of cognitive impairment in schizophrenia and Alzheimer's disease. Working memory deficit in MK-801-treated mice and visual learning deficit in neonatally phencyclidine (PCP)-treated mice were both attenuated by ASP2535 (0.3-3mg/kg, p.o. and 0.3-1mg/kg, p.o., respectively). ASP2535 (1-3mg/kg, p.o.) also improved the PCP-induced deficit in prepulse inhibition in rats. Moreover, the working memory deficit in scopolamine-treated mice and the spatial learning deficit in aged rats were both attenuated by ASP2535 (0.1-3mg/kg, p.o. and 0.1mg/kg, p.o., respectively). These studies provide compelling evidence that ASP2535 is a novel and centrally-active GlyT1 inhibitor that can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease, suggesting that ASP2535 may satisfy currently unmet medical needs for the treatment of these diseases.