EOS789 is an orally active sodium-dependent phosphate transporter inhibitor, with IC 50 values of 6.8, 1.5, and 1.7 μM against human NaPi-IIb, PiT-1, PiT-2 , respectively; and IC 50 values of 3.9, 1.9, and 1.7 μM against rat NaPi-IIb, PiT-1, PiT-2 , respectively. EOS789 inhibits intestinal phosphate absorption, increases fecal phosphate excretion, reduces urinary phosphate excretion, and decreases the levels of serum phosphate, FGF23, and adult parathyroid hormone. EOS789 ameliorates ectopic thoracic aortic calcification, renal injury and hyperphosphatemia, and inhibits the expression of fibrosis markers. EOS789 can be used for the research of hyperphosphatemia and chronic kidney disease-mineral and bone disorder (CKD-MBD).
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