簡(jiǎn)介:LY-411575是高效的 γ-secretase 抑制劑,能夠抑制 Aβ40 蛋白的產(chǎn)生,其 IC50 值為 0.078 nM/0.082 nM(基于膜/細(xì)胞),同時(shí)抑制 Notch 分裂,IC50 值為 0.39 nM。
LY-411575物理化學(xué)性質(zhì):
密度 |
1.4±0.1 g/cm3 |
沸點(diǎn) |
836.0±65.0 °C at 760 mmHg |
分子式 |
C26H23F2N3O4 |
分子量 |
479.475 |
閃點(diǎn) |
459.4±34.3 °C |
精確質(zhì)量 |
479.165649 |
PSA |
98.74 |
LogP |
4.75 |
外觀性狀 |
white to beige |
蒸汽壓 |
0.0±3.2 mmHg at 25°C |
折射率 |
1.652 |
儲(chǔ)存條件 |
﹣20°C |
水溶解性 |
DMSO: soluble5mg/mL, clear |
LY-411575詳細(xì)介紹:
中文名稱: |
(aS)-N-[(1S)-2-[[(7S)-6,7-二氫-5-甲基-6-氧代-5H-二苯并[b,d]氮雜卓-7-基]氨基]-1-甲基-2-氧代乙基]-3,5-二氟-alpha-羥基苯乙酰胺 |
中文別名: |
(aS)-N-[(1S)-2-[[(7S)-6,7-二氫-5-甲基-6-氧代-5H-二苯并[b,d]氮雜卓-7-基]氨基]-1-甲基-2-氧代乙基]-3,5-二氟-alpha-羥基苯乙酰胺;(αS)-N-[(1S)-2-[[(7S)-6,7-二氫-5-甲基-6-氧-5H-二苯并[b,d]氮雜平-7-基]氨基]-1-甲基-2-氧乙基]-3,5-二氟-α-羥基-苯乙酰胺;LY411575 抑制劑 |
英文名稱: |
LY-411575 |
英文別名: |
(aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide;LY 411575;LY-411575;(2S)-2-[[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]propanamide;(S)-2-((S)-2-(3,5-Difluorophenyl)-2-hydroxyacetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanamide;Benzeneacetamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-α-hydroxy-, (αS)-;LSN-411575;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;LY411575;(2S)-2-[[(2S)-2-(3,5-Difluorophenyl)-2-hydroxyacetyl]amino]-N-[(7S)-5-methyl-6-oxo-7H-benzo[d][3]benzazepin-7-yl]propanamide;AOB2210 |
CAS號(hào): |
209984-57-6 |
分子式: |
C26H23F2N3O4 |
分子量: |
479.48 |
詳細(xì)描述: |
博飛美科提供209984-57-6,LY-411575,Medlife,上?,F(xiàn)貨。Medlife,致力于提供高品質(zhì)、高性價(jià)比小分子化合物的產(chǎn)品。 Medlife小分子化合物大量庫(kù)存,提供超過(guò)2萬(wàn)種的抑制劑、激動(dòng)劑、拮抗劑等產(chǎn)品,是藥物及疾病研究的重要原料供應(yīng)商。 γ分泌酶抑制劑,LY-411575 是高效的 γ-secretase 抑制劑,能夠抑制 Aβ40 蛋白的產(chǎn)生,其 IC50 值為 0.078 nM/0.082 nM(基于膜/細(xì)胞),同時(shí)抑制 Notch 分裂,IC50 值為 0.39 nM。 查詢關(guān)鍵詞:“209984-57-6,LY-411575,PC15650,Medlife,上?,F(xiàn)貨”。 |
LY-411575參考文獻(xiàn):
[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.