TAK-653

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

Osavampator (TAK-653) 是一种新型的 AMPA 受体阳性变构调节剂。Osavampator 以谷氨酸依赖方式选择性结合 AMPA-R，诱导 hGluA1i CHO 细胞 Ca2+ 内流 (EC50 = 3.3 μM)。Osavampator 在许多模型里增强学习和记忆能力。Osavampator 目前正在开发用于治疗抑郁症。

Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.

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Animal Model:Normal rats Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg Administration:Oral gavage (p.o.) Result:Improved the novelty discrimination index (NDI).Animal Model:Poor performing rats Dosage:0.3 mg/kg Administration:Oral gavage (p.o.)Result:Increased correct responses and decreased omissions in the poor performing rats.Animal Model:Fasted monkeyDosage:0.06 mg/kg Administration:Oral gavage (p.o.)Result: Significantly increased delayed match-to-sample (DMTS) accuracy at a 16-s delay interval.Maintained the beneficial effect 24 h after administration.Animal Model:submissive behavior model Dosage:0.1 mg/kg, 1 mg/kg Administration:Oral gavage (p.o.)Result:Led to a significant reduction in dominance levels compared with vehicle treatment starting from the seventh day of treatment and maintained throughout the study period. Had a significant effect in reducing dominance levels at 0.1 and 1 mg/kg.

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Membrane Transporter/Ion Channel

iGluR

iGluR

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1358751-06-0

373.47

C19H23N3O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 12.5 mg/mL (33.47 mM )

CC1=CN2CCS(=O)(=O)N=C2C(=N1)c1ccc(OC2CCCCC2)cc1

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(-20℃)

With Ice Pack

≥ 2 years