1779796-27-8
中文名稱
1779796-27-8
英文名稱
LY2365109 (hydrochloride)
CAS
1779796-27-8
更新日期
2024/10/28 15:49:09
分子式
C22H28ClNO5
分子量
421.92
MOL 文件
1779796-27-8.mol
1779796-27-8 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
儲(chǔ)存條件Inert atmosphere,Store in freezer, under -20°C
溶解度Soluble to 100 mM in DMSO and to 50 mM in ethanol
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
LY2365109 hydrochloride 是一種高效、選擇性的 GlyT1 抑制劑，抑制過(guò)表達(dá) hGlyT1 細(xì)胞攝取谷氨酸的 IC50 值為 15.8 nM.靶點(diǎn)
|
hGlyT1 15.8 nM nM (IC 50 ) |
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. |