产品描述: LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a |
靶点:
hGlyT1:15.8 nM nM (IC50);GlyT |
体内研究:
LY2365109 hydrochloride (0.3-30 mg/kg; p.o.) produces dose-dependent elevations in CSF levels of glycine. LY2365109 hydrochloride increases seizure thresholds in mice. Animal Model: Male Sprague-Dawley rats (250-300 g) Dosage: 0.3 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg, 30 mg/kg Administration: Oral administration Result: Produced dose-dependent elevations in CSF levels of glycine measured 1 h after dosing. |
参考文献:
1. Perry KW 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 Oct;55(5):743-54. 2. Shen HY et al. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology. 2015 Dec;99:554-65. |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.37 ml |
11.851 ml |
23.701 ml |
5 mM |
0.474 ml |
2.37 ml |
4.74 ml |
10 mM |
0.237 ml |
1.185 ml |
2.37 ml |
50 mM |
0.047 ml |
0.237 ml |
0.474 ml |
|
注意: |
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