| Size | Price | Stock | Qty |
|---|---|---|---|
| 1kg |
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| Other Sizes |
| Targets |
Ferric citrate targets dietary phosphate in the gastrointestinal tract, binding to it to form insoluble complexes that are excreted in the feces. This reduces serum phosphorus levels in patients with CKD. Ferric citrate also provides iron, which is absorbed and used for hemoglobin synthesis. It is also a Class 1 ferroptosis inducer.
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|---|---|
| ln Vitro |
Iron(III) citrate, or ferric citrate; 1 mM; 24 hr) dramatically causes CM cell death[1]. (CM) cells in a way that is dependent on dosage[1].
In vitro, ferric citrate is used as a ferroptosis inducer in cell culture. It induces iron-dependent oxidative cell death. It is also studied for its effects on iron metabolism and phosphate binding in simulated gastrointestinal conditions. |
| ln Vivo |
Here, we used age-matched wild-type mice and the Col4a3 deletion mouse model of progressive chronic kidney disease to examine the effects of ferric citrate (25 μg/g) supplementation against a mineral-sufficient control diet. For four weeks starting at six weeks of age when the knockout mice had overt chronic renal disease (CKD), or for six weeks starting at four weeks of age when the mice had early CKD, ferric citrate is administered to the mice. Regardless of when treatment is started, ferric citrate reverses iron shortage and anemia in knockout mice, and it also lowers the levels of FGF23 in the blood and on the bone. Additionally, ferric citrate enhances heart health and increases survival rates noticeably[3]. Ferric citrate is a safe and effective phosphate binder that preserves hemoglobin while increasing iron storage, decreasing the need for intravenous iron, reducing erythropoietin-stimulating drug use. Serum ferritin, hemoglobin, and transferrin saturation can all be raised by ferric citrate[2].
In vivo, ferric citrate (Zerenex) is a safe and effective phosphate binder that preserves hemoglobin while increasing iron storage, decreasing the need for intravenous iron, and reducing erythropoietin-stimulating drug use. It is approved for the treatment of iron deficiency anemia in patients with CKD. |
| Enzyme Assay |
Cell-free assays for ferric citrate are not typical, as its mechanism of action is based on phosphate binding in the gastrointestinal tract. Phosphate binding capacity can be measured in vitro by incubating ferric citrate with phosphate-containing solutions and measuring the remaining free phosphate.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Cardiomyocyte (CM) cells Tested Concentrations: 1 mM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically induced CM cell death. In vitro cellular assays for ferric citrate involve treating cells with the compound to study ferroptosis. Cell viability, lipid peroxidation, and iron levels are measured to assess the induction of ferroptosis. |
| Animal Protocol |
In vivo animal studies for ferric citrate are conducted in rodent models of CKD or anemia. The compound is administered orally, and its effects on serum phosphorus, hemoglobin, and iron stores are measured. Iron deposition is observed in various tissues following chronic treatment.
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| ADME/Pharmacokinetics |
Ferric citrate acts locally in the gastrointestinal tract, with minimal systemic absorption. Following absorption, citrate is converted into bicarbonate by the tissues. Formal pharmacokinetic studies have not been performed. The no-observed-adverse-effect level (NOAEL) in dogs was 400 mg/kg/day.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Lactation Use Iron is a normal component of breast milk. Studies on various forms of iron have shown that exogenous supplementation does not significantly increase the iron content in breast milk. No special attention is required. For more information on iron use during lactation, please refer to the monograph on iron salts. ◉ Effects on Breastfed Infants No relevant published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No relevant published information found as of the revision date. Ferric citrate is generally well-tolerated. Common adverse effects include gastrointestinal symptoms such as diarrhea, nausea, and constipation. Iron deposition in tissues has been observed in animal studies. The safety profile is acceptable for its approved indications. |
| References |
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| Additional Infomation |
See also: Iron cations (with active moiety).
Drug indications Fexeric is indicated for the control of hyperphosphatemia in adult patients with chronic kidney disease (CKD). Ferric citrate (Zerenex) is FDA-approved for the control of serum phosphorus levels in patients with chronic kidney disease on dialysis. It is also approved for the treatment of iron deficiency anemia in adults with CKD not on dialysis. Its mechanism involves phosphate binding and iron supplementation. Clinical trials have demonstrated its efficacy in reducing serum phosphorus and increasing hemoglobin levels. |
| Molecular Formula |
C6H5FEO7
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|---|---|
| Molecular Weight |
244.94
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| Exact Mass |
244.938
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| CAS # |
3522-50-7
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| Related CAS # |
Citric acid;77-92-9;Citric acid monohydrate;5949-29-1
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| PubChem CID |
61300
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| Appearance |
Brown to black solid powder
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| Density |
1.762g/cm3
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| Boiling Point |
309.6ºC at 760 mmHg
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| Flash Point |
155.2ºC
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| Vapour Pressure |
5.73E-05mmHg at 25°C
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| Index of Refraction |
1.575
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
211
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NPFOYSMITVOQOS-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/C6H8O7.Fe/c7-3(8)1-6(13,5(11)12)2-4(9)10;/h13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);/q;+3/p-3
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| Chemical Name |
2-hydroxypropane-1,2,3-tricarboxylate;iron(3+)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 5 mg/mL (20.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (40.83 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0826 mL | 20.4132 mL | 40.8263 mL | |
| 5 mM | 0.8165 mL | 4.0826 mL | 8.1653 mL | |
| 10 mM | 0.4083 mL | 2.0413 mL | 4.0826 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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