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My CartCAS：209984-57-6
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 209984-57-6 |
| Name | LY-411575 |
| Molecular Formula | C26H23F2N3O4 |
| Molecular Weight | 479.48 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD09832551 |
| SMILES | C[C@@H](C(=O)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)[C@H](C4=CC(=CC(=C4)F)F)O |
| Target Point | Apoptosis;Notch; -secretase |
| Passage | Apoptosis;Stem Cells;Neuronal Signaling;Stem Cells |
| Background | LY411575, a potent γ-secretase inhibitor, also inhibits Notch fission. |
| Biological Activity | LY-411575 是高效的 γ-secretase 抑制剂，能够抑制 Aβ40 蛋白的产生，其 IC50 值为 0.078 nM/0.082 nM（基于膜/细胞），同时抑制 Notch 分裂，IC50 值为 0.39 nM。[1-5] |
| In Vitro | LY-411，575阻断Notch活化，并导致原代和永生化KS细胞凋亡。 LY-411，575(500μM)诱导G2 / M生长阻滞SLK细胞[2]。 LY411575处理显著降低细胞内HCV RNA的量，IC50为0.56±0.20μM，细胞外HCV颗粒。单独或与达卡他韦(0-40pM)组合的LY411575(0-40nM)以剂量依赖性方式降低上清液感染滴度，并且在感染性病毒的产生方面具有协同作用。 LY411575(10μM)处理会损害HCVcc感染细胞中的ROS产生[4]。 LY411575通过抑制体外Notch信号激活显著减弱EMT [5]。 |
| In Vivo | 当长期给予TgCRND8小鼠时，LY-411，575(10mg / kg)可以大大降低脑和血浆Aβ40和-42 [1]。 LY411，575减少年轻转基因CRND8小鼠(ED50约0.6mg / kg)中的皮质Aβ40，并且在较高剂量(> 3mg / kg)下产生显著的胸腺萎缩和肠杯状细胞增生。 LY411，575(10 mg / kg)诱导肠杯状细胞增生的程度在年轻和老年小鼠中相似[3]。 LY411575抑制体内小鼠增殖性玻璃体视网膜病变(PVR)的形成[5]。 |
| Animal Experiment | 来自老年人群(16-26个月大)的小鼠是退休的育种者或实验性幼稚小鼠。在开始给药之前和研究期间，将小鼠单独用塑料冰屋和筑巢材料饲养。在最后给药后2至4小时处死小鼠。对于口服给药，将LY411，575和LY-D配制成10mg / mL溶液，并用0.4％甲基纤维素1:10稀释。在皮下给药的情况下，将10mg / mL储备溶液用20％羟基 - 丙基-β-环糊精1:10稀释。如有必要，使用适当的1:10载体从1 mg / mL溶液中进行连续稀释。剂量体积为10 mL / kg。口服10mg / kg LY411，575后，给药后血浆Aβ的抑制仍然显著24，但不是48小时，因此为了维持连续的γ-分泌酶抑制，LY411，575和LY-D给药所有研究中每天一次。 |
| Data Literature Source | [1]. Wong GT，et al. Chronic treatment with the gamma-secretase inhibitor LY-411，575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem. 2004 Mar 26;279(13):12876-82. [2]. Curry CL，et al. Gamma secretase inhibitor blocks Notch activation and induces apoptosis in Kaposi's sarcoma tumor cells. Oncogene. 2005 Sep 22;24(42):6333-44. [3]. Hyde LA，et al. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3，5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6，7-dihydro-5H-dibenzo[b，d]azepin-7-yl]-L-alaninamide (LY411，575) in the CRND8 mouse. J Pharmacol Exp Ther. 2006 Dec;319(3):1133-43. [4]. Otoguro T，et al. Inhibitory effect of presenilin inhibitor LY411575 on maturation of hepatitis C virus core protein，production of the viral particle and expression of host proteins involved in pathogenicity. Microbiol Immunol. 2016 Nov;60(11):740-753 [5]. Zhang J，et al. Notch signaling modulates proliferative vitreoretinopathy via regulating retinal pigment epithelial-to-mesenchymal transition. Histochem Cell Biol. 2017 Mar;147(3):367-375. |
| Unit | Bottle |
| Specification | 5mg 10mg |
LY411575是一种有效的γ-secretase抑制剂，也抑制Notch分裂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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