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| Other Sizes |
| Targets |
The primary target of Eprodisate is the interaction between amyloidogenic proteins and glycosaminoglycans. By binding to glycosaminoglycan-binding sites on amyloid proteins, it disrupts the polymerization of amyloid fibrils and their deposition in tissues. This mechanism is designed to interfere with the pathogenesis of amyloidosis.
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| ln Vitro |
In vitro, Eprodisate inhibits the aggregation of amyloid fibrils. It disrupts the interaction between amyloidogenic proteins and glycosaminoglycans. Its activity is assessed by measuring the inhibition of fibril formation using Thioflavin T fluorescence or other amyloid detection methods.
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| ln Vivo |
In vivo, Eprodisate slows the progression of renal disease associated with AA amyloidosis. It has been investigated clinically for treating AA amyloidosis. By preventing amyloid deposition in tissues, it helps preserve organ function, particularly in the kidneys.
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| Enzyme Assay |
For amyloid fibril formation assays, amyloidogenic proteins (e.g., serum amyloid A) are incubated with varying concentrations of Eprodisate. Fibril formation is monitored by Thioflavin T fluorescence or by electron microscopy. The compound's ability to inhibit fibril formation is quantified.
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| Cell Assay |
For cellular studies, cell lines that produce amyloid proteins are cultured. Eprodisate is added to the culture medium. The amount of amyloid deposited in the extracellular matrix is measured by immunofluorescence or ELISA. Cell viability and inflammatory markers are also assessed.
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| Animal Protocol |
For in vivo efficacy studies, animal models of AA amyloidosis are used. Eprodisate is formulated in vehicle and administered orally or intraperitoneally. Amyloid deposition in tissues (e.g., spleen, kidney) is measured by histopathological examination (e.g., Congo red staining). Organ function (e.g., renal function) is assessed by measuring serum creatinine and BUN.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Eprodisate indicate that it is orally active. It is absorbed and distributed to tissues where amyloid deposition occurs. Its metabolism and excretion pathways have been characterized in clinical studies. Its PK profile supports its use for treating systemic amyloidosis.
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| Toxicity/Toxicokinetics |
Toxicological data for Eprodisate are derived from clinical studies. It is generally well-tolerated. No significant organ toxicity has been reported. As with all drugs, it should be used with caution, and appropriate safety precautions should be taken during handling.
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| Additional Infomation |
Eprodishart can slow the decline in renal function in patients with atopic muscular dystrophy (AA).
Drug Indications It has been studied for the treatment of amyloidosis. Mechanism of Action Eprodishart (Kiacta) is a drug that inhibits the deposition of amyloid protein complexes in tissues, thus slowing the decline in renal function associated with AA amyloidosis. AA amyloidosis is a serious, often fatal disease characterized by the deposition of amyloid fibrils in various organs and tissues. It is a complication of many chronic inflammatory diseases, but its etiology and natural course are poorly understood. Eprodishart can slow the progression of kidney disease associated with AA amyloidosis. Eprodisate (CAS 21668-77-9) is an amyloid inhibitor that interferes with the interaction between amyloidogenic proteins and glycosaminoglycans. It has the molecular formula C₃H₈O₆S₂ and a molecular weight of 204.22. It is used to study AA amyloidosis and is strictly for research use. |
| Molecular Formula |
C₃H₈O₆S₂
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|---|---|
| Molecular Weight |
204.22
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| Exact Mass |
203.976
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| CAS # |
21668-77-9
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| Related CAS # |
21668-77-9;36589-58-9 (Sodium);36589-58-9 (Disodium);
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| PubChem CID |
428573
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.8±0.1 g/cm3
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| Melting Point |
120-124ºC
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| Index of Refraction |
1.549
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| LogP |
-3.47
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
11
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| Complexity |
254
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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[H])(=O)(=O)O[H]
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| InChi Key |
MGNVWUDMMXZUDI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C3H8O6S2/c4-10(5,6)2-1-3-11(7,8)9/h1-3H2,(H,4,5,6)(H,7,8,9)
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| Chemical Name |
propane-1,3-disulfonic acid
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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 |
| 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) |
DMSO : ≥ 125 mg/mL (~612.09 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8967 mL | 24.4834 mL | 48.9668 mL | |
| 5 mM | 0.9793 mL | 4.8967 mL | 9.7934 mL | |
| 10 mM | 0.4897 mL | 2.4483 mL | 4.8967 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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