ASP2535

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性、脑渗透性、口服甘氨酸转运蛋白 1 (GlyT1) 抑制剂，IC50 为 92 nM（大鼠 GlyT1），选择性是 GlyT2 的 50 倍。

A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2; shows minimal affinity for many other receptors except for μ-opioid receptors (IC50=1.83 uM); inhibits ex vivo [(3)H]-glycine uptake in mouse cortical homogenate, improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease.Schizophrenia Phase 1 Discontinued.

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

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. Animal Model:5-week-old male ddY mice Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg Administration:Oral administration Result:Significantly attenuated the MK-801-induced decrease in alternation rate.

ASP 2535 | ASP-2535

Membrane Transporter/Ion Channel

GlyT

GlyT

Neurological Disease

Schizophrenia

374886-51-8

382.427

C22H18N6O

>98% (HPLC)

——

CC(C1=NN=C(C2=CC=C(C3=CC=CC=C3)N=C2)N1C4=CC=CC5=NON=C54)C

4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole

(-20℃)

With Ice Pack

≥ 2 years