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LY-411575

    
99.3%

LY-411575

源葉(MedMol)
S80533 一鍵復制產品信息
209984-57-6
C26H23F2N3O4
479.48
MFCD09832551
LY-411575
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S80533-5mg
99.3% ¥586.50 6 - - -
S80533-10mg
99.3% ¥841.50 5 - - -
S80533-25mg
99.3% ¥1683.00 6 - - -
S80533-100mg
≥98% ¥4900.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

LY-411575 是高效的 γ-secretase 抑制劑,能夠抑制 Aβ40 蛋白的產生,其 IC50 值為 0.078 nM/0.082 nM(基于膜/細胞),同時抑制 Notch 分裂,IC50 值為 0.39 nM。

產品描述:

LY-411575 是高效的 γ-secretase 抑制劑,能夠抑制 Aβ40 蛋白的產生,其 IC50 值為 0.078 nM/0.082 nM(基于膜/細胞),同時抑制 Notch 分裂,IC50 值為 0.39 nM。

靶點: 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
體外研究: 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.
體內研究: 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.
參考文獻: 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
保存條件: -20℃
配置溶液濃度參考:
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: 部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。

參考文獻

質檢證書(COA)

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批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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