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EOS789

Chemical Structure : EOS789

CAS No.: 1628848-73-6

EOS789 (EOS 789)

Catalog No.: PC-73328Not For Human Use, Lab Use Only.

EOS789 is a potent, pan-phosphate transporter inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

EOS789 is a potent, pan-phosphate transporter inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively.
EOS789 also inhibited phosphate uptake in normal rat intestinal brush border membrane vesicles with IC50 of 3.1 uM, also inhibited human or rat NaPi-IIa and NaPi-IIc.
EOS789 suppressed intestinal phosphorus absorption via the inhibition of intestinal phosphate transporters in rats.
EOS789 dose-dependently decreased the serum phosphorus concentration in rats with adenine-induced hyperphosphatemia, also dose-dependently decreased the serum FGF-23 and intact PTH concentration.
EOS789 significantly suppressed serum phosphate, FGF-23, and intact PTH levels in CKD-MBD in chronic anti-Thy1.1 nephritis rats.

Physicochemical Properties

M.Wt 772.697
Formula C35H36F8N6O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-(2,3-difluoro-4-(2-((2-methoxyethyl)(methyl)amino)ethoxy)benzyl)-10-hydroxy-6-methyl-8-oxo-N-(4-(trifluoromethyl)-2-(6-(trifluoromethyl)pyrimidin-4-yl)phenyl)-6,7-diazaspiro[4.5]dec-9-ene-9-carboxamide

References

1. Tsuboi Y, et al. Kidney Int. 2020 Aug;98(2):343-354.

2. Hill Gallant KM, et al. Kidney Int. 2021 May;99(5):1225-1233.

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