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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Phosphate Transporter-EOS789 tosylate
EOS789 tosylate

Chemical Structure : EOS789 tosylate

CAS No.: 2460804-35-5

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EOS789 tosylate (EOS 789)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 944.895
分子式 C42H44F8N6O8S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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 tosylate

参考文献

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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