Ko 143
产品说明书
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同义名 : | - |
| CAS号 : | 461054-93-3 | |
| 货号 : | A414772 | |
| 分子式 : | C26H35N3O5 | |
| 纯度 : | 99+% | |
| 分子量 : | 469.57 | |
| MDL号 : | MFCD11042273 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(223.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Ko 143, a potent inhibitor specific to ATP-binding cassette subfamily G member 2 (ABCG2/BCRP), exhibits over 200-fold selectivity against P-gp and MRP-1 transporters[1][2]. At a concentration of 10 nM, Ko 143 notably reduces the IC50 of MTX for HEK G2 cells and mouse G2 cells by 2.5 times. However, Ko143 metabolites, ranging from 1-100 μM, do not affect the function of ABC Transporters[1]. The drug resistance reversal in Topotecan-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells is achieved by the FTC analogue Ko 143, applied at 0, 1, or 8 times the EC90 concentration of 25 nM[2]. Ko 143 also blocks the BCRP-mediated transport of ZD 4522 in both wild type Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC cells and mutant MDCK2-BCRP421AA cells[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.65mL 2.13mL 1.06mL |
21.30mL 4.26mL 2.13mL |
| 参考文献 |
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