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化工產(chǎn)品目錄
生物化工
抑制劑
蛋白酶體(Proteases)
Gamma-secretase 抑制劑
(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
化合物 LY411575
化合物 LY411575|T6063
價(jià)格
¥
338
¥
482
¥
822
包裝
1mg
2mg
5mg
最小起訂量
1mg
發(fā)貨地
上海
更新日期
2024-09-15
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產(chǎn)品詳情
中文名稱:
化合物 LY411575
英文名稱:
LY-411575
CAS:
209984-57-6
品牌:
TargetMol
產(chǎn)地:
美國
保存條件:
keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格:
99.38%
產(chǎn)品類別:
抑制劑
貨號:
T6063
2024-09-15
化合物 LY411575
LY-411575
1mg/338RMB;2mg/482RMB;5mg/822RMB
338
TargetMol
美國
keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
99.38%
抑制劑
Product Introduction
Bioactivity
名稱
LY-411575
描述
LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.
細(xì)胞實(shí)驗(yàn)
DNA/PI staining is performed using standard methodologies. Briefly, 1 × 106 cells are permeabilized with 100% ethanol in the presence of 15% FBS. The cells are washed and then treated for 15 minutes at 37 °C with 10 mg/mL RNAse. PI (5 mg/mL) is added, and the cells incubated for 1 hour at 4 °C prior to analysis by flow cytometry with 10 000 cells analysed per gated determination. The results are confirmed using the Immunotech Annexin V staining kit following the manufacturers’ instructions. At least three independent experiments are performed showing similar results.
激酶實(shí)驗(yàn)
Assays for Aβ and NICD: Procedures for measuring γ-secretase activity in membranes prepared from HEK293 cells expressing APP have been described previously (Zhang L et al Biochemistry 40, 5049-5055). Intact HEK293 cells expressing either APP or NΔE are treated with various concentrations of LY- 411,575 for 4 hours at 37 °C. In the case of cells expressing NΔE, cells are lysed, the cell lysates are separated on a 4-12% NuPAGE gel, and the processed NICD fragment is detected via Western blot with a cleavage site-specific antibody. The inhibition of NICD production is quantified by spot densitometric analysis using FluorChem. In the case of cells expressing APP, the conditioned medium is collected, centrifuged at 10,000 × g for 5 minutes to remove cell debris, and stored at -20 °C prior to the determination of Aβ levels. Aβ40 and -42 produced in HEK293 membrane- and cell-based assays, as well as plasma Aβ40 and cortex Aβ40 from TgCRND8 mice, are analyzed without pretreatment using an electrochemiluminescence detection-based immunoassay. Plasma Aβ42 is measured by enzyme-linked immunosorbent assay. A commercially available enzyme-linked immunosorbent assay kit is used to measure cortex Aβ42 according to the manufacturer''s instructions.
體外活性
LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage. [1] LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells. [2]
體內(nèi)活性
10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. [1] LY-411575 reduces cortical Aβ40 in young (preplaque) transgenic CRND8 mice (ED50 ≈ 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The therapeutic window is similar after oral and subcutaneous administration and in young and aged CRND8 mice. Both the thymus and intestinal side effects are reversible after a 2-week washout period. Three-week treatment with 1 mg/kg LY411575 reduces cortical Aβ40 by 69% without inducing intestinal effects, although a previously unreported change in coat color is observed. [3]
存儲(chǔ)條件
keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 88 mg/mL (183.5 mM)
Ethanol : 11 mg/mL (22.9 mM)
關(guān)鍵字
LY-411575 | Inhibitor | Gamma secretase | γ-secretase | Apoptosis | Notch | LY 411575 | inhibit
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相關(guān)庫
抑制劑庫 | 抗乳腺癌化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗阿爾茨海默癥化合物庫 | HIF-1化合物庫 | 癌細(xì)胞分化化合物庫 | 神經(jīng)退行性疾病化合物庫 | 神經(jīng)元分化化合物庫 | 抗前列腺癌化合物庫
關(guān)鍵字:
LY411575|TargetMol
公司簡介
上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起,為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部,化學(xué)事業(yè)部,生物事業(yè)部和新材料部。 從虛擬篩選到實(shí)體化合物分子供應(yīng);從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成;從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選,從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化,我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。 經(jīng)過在中國市場五年的精心耕耘,我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商,為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩
成立日期
2013-04-18
(12年)
注冊資本
566.2651萬人民幣
員工人數(shù)
100-500人
年?duì)I業(yè)額
¥ 1億以上
主營行業(yè)
化學(xué)試劑,生物活性小分子
經(jīng)營模式
貿(mào)易,試劑,定制,服務(wù)
TargetMol中國(陶術(shù)生物)
VIP
12年
公司成立:
12年
注冊資本:
566.2651萬人民幣
企業(yè)類型:
有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品:
小分子抑制劑,藥物篩選化合物庫,天然產(chǎn)物,活性分子化合物等
公司地址:
上海市閘北區(qū)江場三路28號4樓
進(jìn)入店鋪
詢盤
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化合物 LY411575|T6063相關(guān)廠家報(bào)價(jià)
產(chǎn)品名稱
價(jià)格
公司名稱
報(bào)價(jià)日期
(S)-2-((S)-2-(3,5-二氟苯基)-2-羥基乙酰氨基)-N-((S)-5-甲基-6-氧代-6,7-二氫-5H-二苯并[b,d]氮雜卓-7-基)丙酰胺209984-57-6
詢價(jià)
VIP
3年
河南威梯?;た萍加邢薰?/div>
2024-11-07
209984-57-6LY-411575
詢價(jià)
VIP
3年
上海嘉定區(qū)澄瀏公路52號
2024-11-06
aladdin 阿拉丁 L125846 LY-411575 209984-57-6 ≥98%
¥7209.90
VIP
13年
上海阿拉丁生化科技股份有限公司
2024-10-31
LY-411575
¥900
南京百鑫德諾生物科技有限公司
2024-09-26
aladdin 阿拉丁 L409285 LY411575 209984-57-6 10mM in DMSO
¥888.90
VIP
1年
上海阿拉丁生化科技股份有限公司
2024-08-16
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