| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| F425320-1ml |
1ml |
现货  |
|
| 英文别名 | Daporinad | 658084-64-1 | FK866 | FK-866 | APO-866 | APO866 | 201034-75-5 | FK 866 | Daporinad [INN] | APO 866 | (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide | (E)-N-(4-(1-BENZOYLPIPERIDIN-4-YL)BUTYL)-3-(PYRIDIN-3-YL)ACRYLAMIDE | FK866 hydrochloride hydr |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | FK866 (APO866, Daporinad) |
| 生化机理 | 研究表明，FK-866 可通过对烟酰胺磷酸核糖转移酶 (NAMPT) 的非竞争性和特异性抑制来诱导细胞凋亡。NAMPT 是一种介导细胞内 NAD+ 生物合成的关键调节酶。机理研究表明，该化合物含有一个针对烟酰胺结合和抑制进行了优化的维司他丁酶活性位点。Visfatin 还含有与胰岛素相似的结构，并通过与胰岛素受体结合来模拟胰岛素的作用。在体内具有抗癌活性。口服活性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 烟酰胺磷酸核糖转移酶抑制剂 |
| 产品介绍 |
FK866 (APO866, Daporinad)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase)，无细胞试验中IC50为0.09 nM。Phase 1/2。 FK866 (APO866, Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2. |
| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide |
| INCHI | InChI=1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+ |
| InChi Key | KPBNHDGDUADAGP-VAWYXSNFSA-N |
| Canonical SMILES | C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3 |
| Isomeric SMILES | C1CN(CCC1CCCCNC(=O)/C=C/C2=CN=CC=C2)C(=O)C3=CC=CC=C3 |
| 分子量 | 391.51 |
| Reaxy-Rn | 11331043 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11331043&ln= |
| 敏感性 | 易吸湿 |
|---|---|
| 分子量 | 391.500 g/mol |
| XLogP3 | 3.700 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 3 |
| 可旋转键计数Rotatable Bond Count | 8 |
| 精确质量Exact Mass | 391.226 Da |
| 单同位素质量Monoisotopic Mass | 391.226 Da |
| 拓扑极表面积Topological Polar Surface Area | 62.300 Ų |
| 重原子数Heavy Atom Count | 29 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 534.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 1 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 1 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
| 1. Xinyi Lu, Pingping Jin, Qianyun Tang, Min Zhou, Hanjie Xu, Chen Su, Lei Wang, Feng Xu, Min Zhao, Yongxiang Yin, Jinqiu Zhang, Zhen Jia, Xinrui Peng, Jie Zhou, Lu Wang, Yan Chen, Min Wang, Min Yang, Daozhen Chen, Yu Chen. (2025) NAD+ Metabolism Reprogramming Drives SIRT1-Dependent Deacetylation Inducing PD-L1 Nuclear Localization in Cervical Cancer. Advanced Science, (2412109). [PMID:39988985] [10.1002/advs.202412109] |
| 2. Gui Tianxiang, Liu Ying, Fu Mingfeng, Wu Han, Su Pan, Feng Xuhui, Zheng Mengmeng, Huang Zixuan, Luo Xudong, Boron Walter F., Chen Li-Ming. (2025) Redox state of NAD modulates the activation of Na-bicarbonate cotransporter NBCe1-B via IRBIT and L-IRBIT. Science China-Life Sciences, (1-11). [PMID:39985648] [10.1007/s11427-024-2750-0] |
| 1. Xinyi Lu, Pingping Jin, Qianyun Tang, Min Zhou, Hanjie Xu, Chen Su, Lei Wang, Feng Xu, Min Zhao, Yongxiang Yin, Jinqiu Zhang, Zhen Jia, Xinrui Peng, Jie Zhou, Lu Wang, Yan Chen, Min Wang, Min Yang, Daozhen Chen, Yu Chen. (2025) NAD+ Metabolism Reprogramming Drives SIRT1-Dependent Deacetylation Inducing PD-L1 Nuclear Localization in Cervical Cancer. Advanced Science, (2412109). [PMID:39988985] [10.1002/advs.202412109] |
| 2. Gui Tianxiang, Liu Ying, Fu Mingfeng, Wu Han, Su Pan, Feng Xuhui, Zheng Mengmeng, Huang Zixuan, Luo Xudong, Boron Walter F., Chen Li-Ming. (2025) Redox state of NAD modulates the activation of Na-bicarbonate cotransporter NBCe1-B via IRBIT and L-IRBIT. Science China-Life Sciences, (1-11). [PMID:39985648] [10.1007/s11427-024-2750-0] |
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