1628848-73-6
Chemical Structure
Atidafonat
Synonym(s): EOS789
- CAS No.: 1628848-73-6
- Formula:C35H36F8N6O5
- Molecular Weight:772.70
IUPAC Name: 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
InChIKey: CCBKKKYZCOBIJN-UHFFFAOYSA-N
SMILES: O=C(NC=1C=CC(=CC1C2=NC=NC(=C2)C(F)(F)F)C(F)(F)F)C=3C(=O)N(N(C)C4(C3O)CCCC4)CC5=CC=C(OCCN(C)CCOC)C(F)=C5F
Biological Activity: Atidafonat is an orally active sodium-dependent phosphate transporter inhibitor, with IC50 values of 6.8, 1.5, and 1.7 μM against human NaPi-IIb, PiT-1, PiT-2, respectively; and IC50 values of 3.9, 1.9, and 1.7 μM against rat NaPi-IIb, PiT-1, PiT-2, respectively. Atidafonat inhibits intestinal phosphate absorption, increases fecal phosphate excretion, reduces urinary phosphate excretion, and decreases the levels of serum phosphate, FGF23, and adult parathyroid hormone. Atidafonat ameliorates ectopic thoracic aortic calcification, renal injury and hyperphosphatemia, and inhibits the expression of fibrosis markers. Atidafonat can be used for the research of hyperphosphatemia and chronic kidney disease-mineral and bone disorder (CKD-MBD)[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Atidafonat | 99.14% | Atidafonat is an orally active sodium-dependent phosphate transporter inhibitor, with IC50 values of 6.8, 1.5, and 1.7 μM against human NaPi-IIb, PiT-1, PiT-2, respectively; and IC50 values of 3.9, 1.9, and 1.7 μM against rat NaPi-IIb, PiT-1, PiT-2, respectively. Atidafonat inhibits intestinal phosphate absorption, increases fecal phosphate excretion, reduces urinary phosphate excretion, and decreases the levels of serum phosphate, FGF23, and adult parathyroid hormone. Atidafonat ameliorates ectopic thoracic aortic calcification, renal injury and hyperphosphatemia, and inhibits the expression of fibrosis markers. Atidafonat can be used for the research of hyperphosphatemia and chronic kidney disease-mineral and bone disorder (CKD-MBD). | ||||||||||||||||||||
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References
- [1]. Tsuboi Y, et al. EOS789, a novel pan-phosphate transporter inhibitor, is effective for the treatment of chronic kidney disease-mineral bone disorder. Kidney Int. 2020;98(2):343-354. [Content Brief]
- [2]. Tsuboi Y, et al. EOS789, pan-phosphate transporter inhibitor, ameliorates the progression of kidney injury in anti-GBM-induced glomerulonephritis rats. Pharmacol Res Perspect. 2022;10(3):e00973. [Content Brief]
