Ko 143

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Chemical Structure| 461054-93-3 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

溶解度 : -
动物实验配方:
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

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

[1]Liu K, Zhu J, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200.

[2]Weidner LD, Zoghbi SS, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93.