货号	规格	价格	上海	北京	珠海	重庆	武汉
S80533-5mg买3赠1	99.30%	￥586.00 S80533-5mg ￥586.00 现货（买3赠1）	6 6	-	-	-	-
S80533-10mg买3赠1	99.30%	￥840.00 S80533-10mg ￥840.00 现货（买3赠1）	3 3	-	-	-	-
S80533-25mg买3赠1	99.30%	￥1680.00 S80533-25mg ￥1680.00 现货（买3赠1）	6 0 6	-	-	-	-
S80533-100mg买3赠1	≥98%	￥4420.00 S80533-100mg ￥4420.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

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。

靶点：

IC50: 0.078 nM (γ-secretase in membrane), 0.082 nM (γ-secretase cell-based), 0.39 nM (Notch S3 cleavage cell-based);Apoptosis;Gamma-secretase

体外研究：

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. LY411575 treatment significantly decreases the amounts of intracellular HCV RNA with IC50 of 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. LY411575 significantly attenuates EMT by inhibiting the Notch signaling activation in vitro.

体内研究：

LY-411,575 (10 mg/kg) decreases brain and plasma Aβ40 and -42 robustly when chronically administered to TgCRND8 mice. LY411,575 reduces cortical Aβ40 in young transgenic CRND8 mice (ED50 appr 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. LY411575 inhibits mouse proliferative vitreoretinopathy (PVR) formation in vivo.

参考文献：

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. 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

3. 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.

4. 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.

5. 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 CRND

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.086 ml	10.428 ml	20.856 ml
5 mM	0.417 ml	2.086 ml	4.171 ml
10 mM	0.209 ml	1.043 ml	2.086 ml
50 mM	0.042 ml	0.209 ml	0.417 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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