| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| K424085-1ml |
1ml |
现货  |
|
| 英文别名 | (3s,6s,12as)-1,2,3,4,6,7,12,12a-octahydro-9-methoxy-6-(2-methylpropyl) 1,4-dioxopyrazino [1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester | Ko143 | Ko-143 | 3-((3S,6S,12aS)-6-Isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydro |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Ko 143 |
| 生化机理 | Ko 143 是一种强效的选择性 ABCG2（乳腺癌抗性蛋白多药转运体，BCRP）抑制剂（EC90 = 26 nM）。它对 P-gp 和 MRP-1 转运体的选择性大于 200 倍。Ko 143 还能增加细胞内药物蓄积，逆转 BCRP 介导的多药耐药性。它是一种强效、选择性 BCRP 抑制剂（EC50 值分别为 23 nM 和 26 nM，用于米托蒽醌和托泊替康在癌细胞系中的输出）。无毒的烟曲霉毒素 C 类似物。 |
| 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 | ABCG2 抑制剂 |
| 产品介绍 |
Ko 143是高活性乳腺癌耐药蛋白多药转运通道（BCRP）抑制剂，EC90为26 nM，比对 P-gp和MRP-1转运通道的抑制性高200倍以上。 Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM), Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. |
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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 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | tert-butyl 3-[(2S,5S,8S)-14-methoxy-2-(2-methylpropyl)-4,7-dioxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-5-yl]propanoate |
| INCHI | InChI=1S/C26H35N3O5/c1-14(2)11-20-23-17(16-8-7-15(33-6)12-19(16)27-23)13-21-24(31)28-18(25(32)29(20)21)9-10-22(30)34-26(3,4)5/h7-8,12,14,18,20-21,27H,9-11,13H2,1-6H3,(H,28,31)/t18-,20-,21-/m0/s1 |
| InChi Key | NXNRAECHCJZNRF-JBACZVJFSA-N |
| Canonical SMILES | CC(C)CC1C2=C(CC3N1C(=O)C(NC3=O)CCC(=O)OC(C)(C)C)C4=C(N2)C=C(C=C4)OC |
| Isomeric SMILES | CC(C)C[C@H]1C2=C(C[C@@H]3N1C(=O)[C@@H](NC3=O)CCC(=O)OC(C)(C)C)C4=C(N2)C=C(C=C4)OC |
| WGK Germany | 3 |
| 分子量 | 469.57 (anhydrous basis) |
| Reaxy-Rn | 11166757 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11166757&ln= |
| 折光率 | 1.6 |
|---|---|
| 沸点 | ~689.8° C at 760 mmHg |
| 熔点 | 294.92°C |
| 分子量 | 469.600 g/mol |
| XLogP3 | 3.500 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 8 |
| 精确质量Exact Mass | 469.258 Da |
| 单同位素质量Monoisotopic Mass | 469.258 Da |
| 拓扑极表面积Topological Polar Surface Area | 101.000 Ų |
| 重原子数Heavy Atom Count | 34 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 794.000 |
| 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 | 3 |
| 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 | 0 |
| 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 | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。 P403+P233: 存放在通风良好的地方。保持容器密闭。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。 P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。 P319: 如果你感到不适，请寻求医疗帮助。 |
| WGK Germany | 3 |
| Reaxy-Rn | 11166757 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11166757&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
| 1. Yanghui Chen, Yuan Li, Junliang Luo, Zixin Li, Yu Huang, Jia Cai, Dongneng Jiang, Defeng Zhang, Jichang Jian, Jun Qiang, Bei Wang. (2024) A novel study of brain microvascular endothelial cells induced by astrocyte conditioned medium for constructing blood brain barrier model in vitro: A promising tool for meningitis of teleost. FISH & SHELLFISH IMMUNOLOGY, 146 (109401). [PMID:38266792] [10.1016/j.fsi.2024.109401] |
| 2. Rui Li, Wenhui Ruan, Rui Hao, Jue Chen, Chu Xu, Liyan Lu, Yingli Wang. (2025) O-carboxymethyl chitosan-grafted-cholesterol succinic acid monoester nanomicelles improve oral absorption of cannabidiol: Preparation, intestinal absorption in vitro, and pharmacokinetics in vivo. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, (106763). [10.1016/j.jddst.2025.106763] |
| 3. Wenqing Sun, Yufeng Xu, Zhiqin Liu, Wei Liu, Hongting Wang, Guanyu Chang, Zihui Yang, Zhen Dong, Jianguo Zeng. (2024) Studies on pharmacokinetic properties and intestinal absorption mechanism of sanguinarine chloride: in vivo and in situ. TOXICOLOGY MECHANISMS AND METHODS, [PMID:39087424] [10.1080/15376516.2024.2383366] |
| 1. Yanghui Chen, Yuan Li, Junliang Luo, Zixin Li, Yu Huang, Jia Cai, Dongneng Jiang, Defeng Zhang, Jichang Jian, Jun Qiang, Bei Wang. (2024) A novel study of brain microvascular endothelial cells induced by astrocyte conditioned medium for constructing blood brain barrier model in vitro: A promising tool for meningitis of teleost. FISH & SHELLFISH IMMUNOLOGY, 146 (109401). [PMID:38266792] [10.1016/j.fsi.2024.109401] |
| 2. Rui Li, Wenhui Ruan, Rui Hao, Jue Chen, Chu Xu, Liyan Lu, Yingli Wang. (2025) O-carboxymethyl chitosan-grafted-cholesterol succinic acid monoester nanomicelles improve oral absorption of cannabidiol: Preparation, intestinal absorption in vitro, and pharmacokinetics in vivo. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, (106763). [10.1016/j.jddst.2025.106763] |
| 3. Wenqing Sun, Yufeng Xu, Zhiqin Liu, Wei Liu, Hongting Wang, Guanyu Chang, Zihui Yang, Zhen Dong, Jianguo Zeng. (2024) Studies on pharmacokinetic properties and intestinal absorption mechanism of sanguinarine chloride: in vivo and in situ. TOXICOLOGY MECHANISMS AND METHODS, [PMID:39087424] [10.1080/15376516.2024.2383366] |
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