Size | Price | Stock |
---|---|---|
5mg | $80 | In-stock |
10mg | $140 | In-stock |
25mg | $280 | In-stock |
50mg | $500 | In-stock |
100mg | $900 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-10010 |
M.Wt: | 469.57 |
Formula: | C26H35N3O5 |
Purity: | >98 % |
Solubility: | DMSO : 100 mg/mL (212.96 mM; Need ultrasonic) |
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[1][2]. 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 SKF 104864A-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 ZD 4522 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 SKF 104864A in mice[2]. Ko143 significantly affects the pharmacokinetics of ZD 4522 in rats[3].
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