| 產(chǎn)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 |
| 靶點(diǎn)： |
hGlyT1:15.8 nM nM (IC50);GlyT |
| 體內(nèi)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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京