2. Membrane Transporter/Ion Channel
  3. Sodium Phosphate Cotransporter
  4. EOS789

EOS789 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. 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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EOS789

EOS789 Chemical Structure

CAS No. : 1628848-73-6

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Based on 1 publication(s) in Google Scholar

EOS789 Related Antibodies

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Description

EOS789 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. 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)[1][2].

In Vitro

EOS789 (various concentrations) inhibits phosphate uptake in normal rat intestinal brush border membrane vesicles with an IC50 of 3.1 μmol/l[1].
EOS789 (0.3-3.0 μM; 24 h) dose-dependently suppresses high phosphate-induced upregulation of Collagen 1A1, Collagen 3A1, and α-smooth muscle actin mRNA in hMes 130hT-9 human mesangial cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EOS789 Related Antibodies

Real Time qPCR[2]

Cell Line: hMes 130hT-9 immortalized human mesangial cells
Concentration: 0.3 μM, 1.0 μM, 3.0 μM
Incubation Time: 24 h
Result: Significantly suppressed Collagen 1A1 relative expression at 1.0 μM and 3.0 μM.
Significantly suppressed Collagen 3A1 relative expression at 1.0 μM and 3.0 μM.
Significantly suppressed α-smooth muscle actin relative expression at 3.0 μM.
Showed a dose-dependent inhibitory effect on all three fibrotic marker genes.
Parmacokinetics
Species Dose Route AUC0-∞ F
Rat[1] 2 mg/kg i.v. 31900 ng·h/mL /
Rat[1] 20 mg/kg p.o. 22000 ng·h/mL 6.9 %
In Vivo

EOS789 (0.050-0.50%; p.o.; daily; 3 days) dose-dependently increases fecal phosphorus excretion, decreases urinary phosphorus excretion, and reduces serum phosphorus levels in normal male Wistar rats, confirming inhibition of intestinal phosphate absorption[1].
EOS789 (0.015-1.0%; p.o.; daily; 14 days) dose-dependently reduces serum phosphate, FGF-23, and intact PTH levels, increases fecal phosphorus excretion, and decreases urinary phosphorus excretion in adenine-induced hyperphosphatemic male Wistar rats, with greater potency than a NaPi-IIb-selective inhibitor at equivalent doses[1].
EOS789 (0.3%; p.o.; ad libitum; day 21 to day 116) sustainably suppresses serum phosphate, FGF-23, and intact PTH levels, ameliorates aortic calcification, reduces serum creatinine, and improves kidney histopathology and fibrotic gene expression in chronic anti-Thy1.1 nephritis male Fisher rats[1].
EOS789 (0.3%; food admixture; ad libitum; 5 weeks) significantly ameliorates hyperphosphatemia, improves kidney function, and reduces glomerular crescent formation in anti-GBM-induced glomerulonephritis rats, with a significant reduction in serum creatinine to 1.31 mg/dL and glomerular crescent formation to 66.1% of total glomeruli[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Crlj:WI (Wistar) (male)[1]
Dosage: 0.050%, 0.15%, 0.50%
Administration: p.o.; daily; 3 days
Result: Increased fecal 33P excretion rate from ~45% to ~55%.
Decreased urinary 33P excretion rate from ~4.5% to ~3%.
Decreased serum 33P radioactivity from ~3900 dpm/mL to ~3500 dpm/mL.
Increased fecal 33P excretion rate to ~60%.
Decreased urinary 33P excretion rate to ~2.2%.
Decreased serum 33P radioactivity to ~3200 dpm/mL.
Increased fecal 33P excretion rate to ~70%.
Decreased urinary 33P excretion rate to ~1.2%.
Decreased serum 33P radioactivity to ~2700 dpm/mL.
Animal Model: Crlj:WI (Wistar) (male, adenine-induced hyperphosphatemia)[1]
Dosage: 0.015%, 0.05%, 0.15%, 0.50%, 1.0%
Administration: p.o.; daily; 14 days
Result: Reduced serum phosphate from 9.7 mg/dl to ~7.5 mg/dl.
Reduced serum FGF-23 from ~10,000 pg/mL to ~1500 pg/mL.
Reduced serum intact PTH from ~700 pg/mL to ~450 pg/mL.
Reduced serum phosphate to ~6.8 mg/dl.
Reduced serum FGF-23 to ~1200 pg/mL.
Reduced serum intact PTH to ~350 pg/mL.
Reduced serum FGF-23 to ~800 pg/mL.
Reduced serum intact PTH to ~400 pg/mL.
Reduced serum FGF-23 to ~150 pg/mL.
Reduced serum intact PTH to ~100 pg/mL.
Reduced serum phosphate to ~6.5 mg/dl.
Increased fecal phosphorus excretion from ~78 mg/4d to ~120 mg/4d.
Decreased urinary phosphorus excretion from ~3.5 mg/d to near 0 mg/d.
Animal Model: F344/DuCrlCrlj (Fisher) (male, anti-Thy1.1-induced chronic kidney disease-mineral bone disorder)[1]
Dosage: 0.1%, 0.3%
Administration: p.o.; ad libitum; day 21 to day 116
Result: Reduced serum phosphate from ~12 mg/dl to ~10 mg/dl at study end.
Did not significantly reduce serum FGF-23 or intact PTH levels.
Showed no significant reduction in aortic calcium content.
Reduced serum phosphate to ~8 mg/dl.
Reduced serum FGF-23 from ~240,000 pg/mL to ~5000 pg/mL.
Reduced serum intact PTH from ~8000 pg/mL to ~4000 pg/mL.
Reduced serum creatinine from ~3.2 mg/dl to ~2.4 mg/dl.
Suppressed aortic calcium content to near normal levels, with no histopathologic calcification observed in any treated rats.
Reduced glomerulosclerosis score from 2.60 to 2.32, degeneration of tubules score from 2.54 to 2.23, and tubulointerstitial fibrosis score from 2.39 to 2.01.
Significantly reduced renal mRNA expression of TGF-β1, collagen type 1 α1, collagen type 3 α1, and α-smooth muscle actin versus disease control (0.3% dose).
Animal Model: Wistar (male, 7 weeks old, anti-rat GBM antibody-induced glomerulonephritis)[2]
Dosage: ~100 mg/kg/day; ~200 mg/kg/day
Administration: food admixture; ad libitum; 5 weeks
Result: Dose-dependently suppressed the disease-induced increase in serum phosphate.
Increased fecal phosphate excretion significantly to 89.1 mg/day.
Decreased fractional urinary phosphate excretion significantly to 18.5%.
Significantly suppressed serum FGF23 increase.
Significantly improved severely reduced serum calcitriol.
Decreased serum creatinine significantly to 1.31 mg/dL.
Decreased urinary fractional excretion of albumin significantly to 0.04%.
Decreased serum sodium significantly to 140.5 mEq/L.
Decreased urinary fractional excretion of sodium significantly to 1.15%.
Decreased glomerular crescent formation significantly to 66.1% of total glomeruli.
Significantly increased body weight compared to disease control.
Clinical Trial
Molecular Weight

772.70

Formula

C35H36F8N6O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (129.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2942 mL 6.4708 mL 12.9416 mL
5 mM 0.2588 mL 1.2942 mL 2.5883 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (3.24 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2942 mL 6.4708 mL 12.9416 mL 32.3541 mL
5 mM 0.2588 mL 1.2942 mL 2.5883 mL 6.4708 mL
10 mM 0.1294 mL 0.6471 mL 1.2942 mL 3.2354 mL
15 mM 0.0863 mL 0.4314 mL 0.8628 mL 2.1569 mL
20 mM 0.0647 mL 0.3235 mL 0.6471 mL 1.6177 mL
25 mM 0.0518 mL 0.2588 mL 0.5177 mL 1.2942 mL
30 mM 0.0431 mL 0.2157 mL 0.4314 mL 1.0785 mL
40 mM 0.0324 mL 0.1618 mL 0.3235 mL 0.8089 mL
50 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.6471 mL
60 mM 0.0216 mL 0.1078 mL 0.2157 mL 0.5392 mL
80 mM 0.0162 mL 0.0809 mL 0.1618 mL 0.4044 mL
100 mM 0.0129 mL 0.0647 mL 0.1294 mL 0.3235 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EOS7891628848-73-6EOS 789EOS-789Sodium Phosphate CotransporterCHO-K1 cellsPiT-1chronic kidney disease-mineral and bone disorderNaPi-IIbNaPi-IIcNaPi-IIahMes 130hT-9 human mesangial cellsWistar ratsFisher ratsPiT-2Inhibitorinhibitorinhibit

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