| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| Other Sizes |
| Targets |
Eprodisate Disodium targets the process of fibrillogenesis, specifically the aggregation and deposition of serum amyloid A protein into amyloid fibrils. As a negatively charged sulfonated molecule, it interferes with the interactions between amyloidogenic proteins that lead to fibril formation and deposition. By inhibiting fibrillogenesis, the compound reduces the accumulation of amyloid deposits in tissues and organs, slowing the progression of organ damage in AA amyloidosis. The compound does not target a specific receptor but rather the physicochemical process of protein aggregation.
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| ln Vitro |
In vitro, Eprodisate Disodium demonstrates inhibition of amyloid fibril formation in biochemical assays using purified serum amyloid A protein or other amyloidogenic proteins. The compound's negatively charged sulfonate groups interact with positively charged regions on amyloidogenic proteins, preventing their aggregation into fibrillar structures. In cell-based assays, Eprodisate reduces amyloid deposition and associated cytotoxicity. The compound's inhibitory activity is concentration-dependent, with efficacy demonstrated at micromolar concentrations.
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| ln Vivo |
In vivo, Eprodisate Disodium has been evaluated in animal models of AA amyloidosis and in clinical trials. In preclinical studies, oral administration of the compound reduces amyloid deposition in various organs and slows the progression of organ dysfunction. Clinical trials have demonstrated that Eprodisate can slow the decline in renal function in patients with AA amyloidosis. The compound has been shown to be effective in reducing the progression of amyloid-related organ damage.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to Eprodisate Disodium as it functions by inhibiting fibrillogenesis rather than binding to a specific enzyme or receptor. Instead, the compound's activity is assessed using amyloid fibril formation assays. Purified serum amyloid A protein or other amyloidogenic proteins are incubated with varying concentrations of Eprodisate under conditions that promote fibril formation. Fibril formation is monitored using thioflavin T fluorescence, which increases upon binding to amyloid fibrils. The compound's ability to inhibit fibril formation is quantified by the reduction in fluorescence.
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| Cell Assay |
In vitro cellular assays for Eprodisate Disodium utilize cell lines or primary cells exposed to amyloidogenic proteins. Cells are treated with amyloidogenic proteins in the presence or absence of Eprodisate, and amyloid deposition is assessed using Congo red staining or immunofluorescence. Cytotoxicity is measured using LDH release or MTT assays to determine whether the compound protects cells from amyloid-induced damage. The compound's effects on cellular uptake and clearance of amyloid proteins may also be assessed.
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| Animal Protocol |
In vivo animal experiments for Eprodisate Disodium typically involve mouse models of AA amyloidosis. Mice are induced to develop AA amyloidosis by injection of inflammatory stimuli (such as silver nitrate or casein) to increase serum amyloid A production. Eprodisate is administered orally at doses ranging from 10 to 100 mg/kg daily for several weeks. Amyloid deposition in spleen, liver, kidney, and other organs is assessed by histopathology and Congo red staining. Organ function is assessed by biochemical markers. The compound's efficacy in reducing amyloid burden and preserving organ function is evaluated.
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| ADME/Pharmacokinetics |
Eprodisate Disodium is orally bioavailable, enabling convenient administration for chronic treatment. Following oral administration, the compound reaches systemic circulation and distributes to various tissues where amyloid deposition occurs. Pharmacokinetic studies have characterized the compound's absorption, distribution, metabolism, and excretion. The compound is not extensively metabolized and is eliminated primarily via renal excretion. Its half-life supports twice-daily or once-daily dosing in clinical settings.
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| Toxicity/Toxicokinetics |
Preclinical and clinical toxicology studies of Eprodisate Disodium have demonstrated an acceptable safety profile. In clinical trials, the compound was generally well-tolerated with no significant dose-limiting toxicities. Common adverse effects were mild and included gastrointestinal disturbances. No significant effects on liver function, hematological parameters, or other organ systems were observed at therapeutic doses. The compound's safety profile supports its use for the chronic treatment of AA amyloidosis.
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| Additional Infomation |
Eprodisate disodium is the oral disodium salt of Eprodisate, a negatively charged sulfonated fibrillary formation inhibitor used to treat AA type amyloidosis. After administration, Eprodisate competitively binds to the glycosaminoglycan binding sites on serum amyloid A (SAA), thereby inhibiting the formation of glycosaminoglycan-amyloid fibrillary aggregates. This prevents the formation of amyloid deposits in certain organs, particularly the kidneys, in patients with AA type amyloidosis.
Eprodisate Disodium is an orally available sulfonated inhibitor of fibrillogenesis developed for the treatment of AA amyloidosis. It has a molecular formula of C3H6Na2O6S2 and a molecular weight of 248.19 g/mol. The compound works by inhibiting the formation of amyloid fibrils from serum amyloid A protein, reducing organ damage. Clinical trials have demonstrated that Eprodisate can slow the decline in renal function in patients with AA amyloidosis. |
| Molecular Formula |
C3H6NA2O6S2
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|---|---|
| Molecular Weight |
248.17
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| Exact Mass |
247.94
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| CAS # |
36589-58-9
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| Related CAS # |
21668-77-9;36589-58-9 (Sodium);36589-58-9 (Disodium);
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| PubChem CID |
6451143
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| Appearance |
White to off-white solid powder
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| Density |
1.773 g/cm3
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| Melting Point |
>300°C
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| LogP |
0.628
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
227
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])C([H])([H])C([H])([H])S(=O)(=O)[O-])(=O)(=O)[O-].[Na+].[Na+]
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| InChi Key |
DKGJFKPIUSHDIT-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C3H8O6S2.2Na/c4-10(5,6)2-1-3-11(7,8)9;;/h1-3H2,(H,4,5,6)(H,7,8,9);;/q;2*+1/p-2
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| Chemical Name |
disodium;propane-1,3-disulfonate
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| Synonyms |
Eprodisate Disodium Kiacta Eprodisate sodium
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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 : ~50 mg/mL (~201.46 mM)
DMSO : ~7.69 mg/mL (~30.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.77 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.77 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.77 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (402.92 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0295 mL | 20.1475 mL | 40.2950 mL | |
| 5 mM | 0.8059 mL | 4.0295 mL | 8.0590 mL | |
| 10 mM | 0.4029 mL | 2.0147 mL | 4.0295 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01215747 | COMPLETED | Drug: KIACTA (eprodisate disodium) Drug: Placebo |
Amyloidosis | C.T. Development America, Inc. | 2010-11 | Phase 3 |
| NCT00675857 | COMPLETED | Drug: NC-503 (eprodisate disodium) Other: placebo |
Diabetes Mellitus, Type 2 Metabolic Syndrome X |
Bellus Health Inc. - a GSK company | 2008-04 | Phase 2 |
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