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LY 2365109 盐酸盐 /LY2365109 HCl {[allProObj[0].p_purity_real_show]}

货号:A826662 同义名: LY2365109 hydrochloride

LY2365109 is a selective inhibitor of GlyT1 with IC50 of 15.8 nM.

LY2365109 HCl 化学结构 CAS号:1779796-27-8
LY2365109 HCl 化学结构
CAS号:1779796-27-8
LY2365109 HCl 3D分子结构
CAS号:1779796-27-8
LY2365109 HCl 化学结构 CAS号:1779796-27-8
LY2365109 HCl 3D分子结构 CAS号:1779796-27-8
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LY2365109 HCl 纯度/质量文件 产品仅供科研

货号:A826662 标准纯度: {[allProObj[0].p_purity_real_show]}
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LY2365109 HCl 生物活性

描述 The glycine transporter 1 (GlyT1) is a target for the treatment of central nervous system disorders related to hypoglutamatergic function. LY2365109 is a selective GlyT1 inhibitor that inhibits [14C] glycine uptake in cells transfected with hGlyT1a with an IC50 value of 15.8 nM. The administration of rats with LY2365109 (0.3 – 30 mg/kg, p.o.) for 1 h led to a dose-dependent elevation in the cerebrospinal fluid level of glycine. LY2365109 at a dose of 3 mg/kg significantly increased NMDA-induced release of dopamine at 1.5h post-dosing relative to the controls. LY2365109 at 10 mg/kg significantly enhanced dopamine release at 1.5 - 2h after treatment. Rats treated with LY2365109 (3 and 10 mg/kg, p.o.) also showed impaired gait with ataxic like behavior and compulsive “toe walking” around the cage at 8h after LY2365109 administration[3].
作用机制 LY2365109 is a sarcosine-like GlyT1 inhibitor that potentiate NMDA function in the prefrontal cortex and mediates sustained inhibition of GlyT1 transporter in the caudal areas of the brain[3].

LY2365109 HCl 参考文献

[1]Shen HY, van Vliet EA, et al. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology. 2015 Dec;99:554-65.

[2]Shen HY, van Vliet EA, et al. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology. 2015 Dec;99:554-65.

[3]Perry KW, Falcone JF, Fell MJ, et al. Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas. Neuropharmacology. 2008;55(5):743-754. doi:10.1016/j.neuropharm.2008.06.016

LY2365109 HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.85mL

2.37mL

1.19mL

23.70mL

4.74mL

2.37mL

LY2365109 HCl 技术信息

CAS号1779796-27-8
分子式C22H28ClNO5
分子量 421.914
别名 LY2365109 hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 30 mg/mL(71.1 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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