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  • 达珀利奈|T2644|TargetMol

达珀利奈|T2644|TargetMol

(E)-Daporinad
658084-64-1
238 1mg 起订
548 5mg 起订
987 10mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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产品详情:

中文名称:
达珀利奈
英文名称:
(E)-Daporinad
CAS号:
658084-64-1
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.96%
产品类别:
抑制剂
货号:
T2644

Product Introduction

Bioactivity

名称(E)-Daporinad
描述(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.
细胞实验For MTT assays, 0.5 × 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5 × 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells. (Only for Reference)
激酶实验High Throughput Screening: FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program.
体外活性方法:用 (E)-Daporinad( FK866 )(100 nM,30 分钟) 预处理肝细胞,然后进行 GaIN/LPS(G/L,1 mg/mL /30 ng/mL,24 小时)攻击,观察(E)-Daporinad( FK866 )是否能减轻GaIN/LPS诱导的肝毒性。 结果:用(E)-Daporinad( FK866 )预处理的原代肝细胞在GaIN/LPS损伤后表现出自噬活性显着增加,(E)-Daporinad( FK866 )可以改善GaIN/LPS和ConA诱导的肝损伤,其保护机制可能涉及其通过抑制JNK诱导自噬的能力。[1]
体内活性方法:用GaIN/LPS和ConA处理小鼠前24、12和0.5小时施用(E)-Daporinad( FK866 )(10mg / kg,腹腔注射),测试(E)-Daporinad( FK866 )对小鼠ALF的潜在影响。 结果:(E)-Daporinad( FK866 )治疗后降低了GaIN/LPS或ConA治疗小鼠的死亡率,(E)-Daporinad( FK866 )处理前和处理后均能减弱小鼠GaIN/LPS和ConA诱导的ALF,且(E)-Daporinad( FK866 )预处理对GaIN/LPS或ConA攻击的响应效果更好。[1]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 50 mg/mL (127.71 mM)
10% DMSO+90% Saline : 0.1 mg/mL (0.26 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol : 72 mg/mL (183.9 mM)
关键字inhibit | Visfatin | (E) Daporinad | FK 866 | Autophagy | Nicotinamide phosphoribosyl transferase | NAMPT | PBEF | APO 866 | Inhibitor | Pre-B cell colony enhancing factor | APO-866 | (E)-Daporinad | (E)Daporinad | FK-866
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相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 代谢化合物库 | 抗衰老化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 人代谢物化合物库 | 抗癌药物库
达珀利奈|||FK866|||Daporinad|||APO866|||(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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