Ko 143 | CAS:461054-93-3

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のKo 143(CAS:461054-93-3)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:Ko 143; 
Cat. No. :CS-0298
CAS No. :461054-93-3
Formula:C26H35N3O5
M. Wt. : 469.57
Solubility:10 mM in DMSO

Ko 143 is a practical breast cancer resistance protein multidrug transporter inhibitor BCRP, with the EC90 value of 26 nM.IC50 & Target: EC90: 26 nM (BCRP)In Vitro: Ko143 (10 nM) significantly decreases (2.5-fold) the IC50 of MTX for HEK G2 cells and mouse G2 cells. Ko143 (1-100 μM) metabolite does not inhibit the function of ABC Transporters[1]. Reversal of drug resistance in topotecan-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by FTC analogue Ko143. Ko143 is applied at zero, one, or eight times the EC90 concentration of 25 nM[2]. Ko143 inhibits BCRP-mediated transport of rosuvastatin in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells[3].In Vivo: Ko143 (10 mg/kg, p.o.) increases the oral availability of topotecan in mice[2]. Ko143 significantly affects the pharmacokinetics of rosuvastatin in rats[3].

Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. 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. 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. Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of Rosuvastatin In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25.