2016年1月27日星期三

Ko 143|Ko143|BCRP inhibitor| DC Chemicals

Ko 143|Ko143|BCRP inhibitor| DC Chemicals

Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM), Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters.

Product Name: Ko 143 |Catalog Number: DC8788 |CAS 461054-93-3 |Other names: Ko-143; Ko143 |Chemical Name:  |Molecule Formular: C26H35N3O5 |MW: 469.57

Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM), Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters.
in vitro:  Ko143 appears to be the most potent BCRP inhibitor known thus far. In contrast, the compounds have only low activity against P-glycoprotein, the multidrug resistance-associated protein (MRP1), or other known drug transporters.
in vivo: Ko 143 is nontoxic in vitro at useful concentrations and evinced no signs of toxicity in mice at high oral or i.p. doses. Administered p.o. to inhibit intestinal Bcrp1, Ko143 markedly increased the oral availability of topotecan in mice.

For research only, not for human use!



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