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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-GW117
GW117

Chemical Structure : GW117

CAS No.: 2260629-83-0

GW117 (GW-117)

货号: PC-22026Not For Human Use, Lab Use Only.

GW117 is a novel serotonin (5-HT2C) receptor antagonist and melatonin (MT1 /MT2 ) receptor agonist with Ki values of 0.32, 0.12, and 54 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GW117 is a novel serotonin (5-HT2C) receptor antagonist and melatonin (MT1 /MT2 ) receptor agonist with Ki values of 0.32, 0.12, and 54 nM, respectively.
GW117 stimulates specific [35S]‐GTPγS binding with an EC50 of 2.49 nM and 1.54 nM and a maximal increase over basal binding (% Emax) of 104 ± 7.34% and 103.2 ± 4.56% on the MT1 receptor and MT2 receptor, respectively.
GW117 dose‐dependently blocked activation of [35S]‐GTPγS binding and [3H]PIP released by 10 nM 5‐HT.
GW117 (20, and 40 mg/kg, p.o.) markedly reduced the immobility time on TST test in mice, showed potential antidepressant‐like activity.

物理化学性质&存储条件

分子量 280.77
分子式 C15H13D3ClNO2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(6-chloro-7-(methoxy-d3)naphthalen-1-yl)ethyl)acetamide

参考文献

1. Gao N, et al. CNS Neurosci Ther. 2021 Jun;27(6):702-713.

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