Chemical Structure : EOS789 tosylate
CAS No.:
2460804-35-5
EOS789 tosylate
(EOS 789)
Catalog No.: PC-73329Not For Human Use, Lab Use Only.
EOS789 tosylate is a potent, pan-phosphate transporter (NaPi-2b, PiT-1, PiT-2) 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 tosylate is a potent, pan-phosphate transporter (NaPi-2b, PiT-1, PiT-2) 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
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M.Wt
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944.895
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Formula
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C42H44F8N6O8S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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 tosylate
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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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