DS-1211 (DS1211) is a potent, selecitve inhibitor of tissue-nonspecific alkaline phosphatase (TNAP) with IC50 of 3.4 nM.
DS-1211 displays >400-fold selectivity over intestinal alkaline phosphatase (IAP) and placental alkaline phosphatase (PLAP), also shows no significant response(≥50% inhibition) on a total of 88 receptors, channels, transporters, and enzymes.
DS-1211 exhibits TNAP selectivity and potent inhibition of TNAP across species.
DS-1211 inhibits ALP activity through an uncompetitive mode of action.
DS-1211 effetively inhibits mouse, monkey, and human plasma alkaline phosphatase with IC50 of 13.3, 36.3 and 28.3 nM, respectively.
Single oral administration of DS-1211 showed linear pharmacokinetics, with dose-dependent inhibition of ALP activity, and increases in plasma PPi and PLP in vivo.
