CAS NO: | 209984-57-6 |
生物活性 | LY-411575 is a potentγ-secretaseinhibitor withIC50of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibitsNotchS3 cleavage withIC50of 0.39 nM. | ||||||||||||||||
IC50& Target | IC50: 0.078 nM (γ-secretase in membrane), 0.082 nM (γ-secretase cell-based), 0.39 nM (Notch S3 cleavage cell-based)[1] | ||||||||||||||||
体外研究 (In Vitro) | LY-411,575 blocks Notch activation, and results in apoptosis in primary and immortalized KS cells. LY-411,575 (500 μM) induces G2/M growth arrest SLK cells[2]. LY411575 treatment significantly decreases the amounts of intracellular HCV RNA with IC50of 0.56 ± 0.20 μM and extracellular HCV particles. LY411575 (0-40 nM) alone or in combination with BMS-790052 (0-40 pM) decreases supernatant infectious titers in a dose-dependent manner, and is synergistic regarding production of infectious virus. LY411575 (10 μM) treatment impairs ROS production in HCVcc-infected cells[4]. LY411575 significantly attenuates EMT by inhibiting the Notch signaling activation in vitro[5]. | ||||||||||||||||
体内研究 (In Vivo) | LY-411,575 (10 mg/kg) decreases brain and plasma Aβ40 and -42 robustly when chronically administered to TgCRND8 mice[1]. LY411,575 reduces cortical Aβ40 in young transgenic CRND8 mice (ED50appr 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The extent of intestinal goblet cell hyperplasia induced by LY411,575 (10 mg/kg) is similar in young and aged mice[3]. LY411575 inhibits mouse proliferative vitreoretinopathy (PVR) formation in vivo[5]. | ||||||||||||||||
分子量 | 479.48 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H23F2N3O4 | ||||||||||||||||
CAS 号 | 209984-57-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(69.51 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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