S83984 |
LY2365109 (hydrochloride) |
源葉(MedMol) | 98% |
- 提示:詳情請下載說明書。
- 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: 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:
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
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