產品描述: | Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters |
靶點: |
EC90: 26 nM (BCRP);BCRP;ABC |
體內研究: |
Ko143 (10 mg/kg, p.o.) increases the oral availability of SKF 104864A in mice. Ko143 significantly affects the pharmacokinetics of ZD 4522 in rats |
參考文獻: |
1. Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. 2. JD Allen et al. Potent and Specific Inhibition of the Breast Cancer Resistance Protein Multidrug Transporter in Vitro and in Mouse Intestine by a Novel Analogue of Fumitremorgin C. Mol. Cancer Ther. 2002, 1, 417-425. 3. Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25. 4. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9. 5. Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.13 ml |
10.648 ml |
21.296 ml |
5 mM |
0.426 ml |
2.13 ml |
4.259 ml |
10 mM |
0.213 ml |
1.065 ml |
2.13 ml |
50 mM |
0.043 ml |
0.213 ml |
0.426 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |