| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Carbonic anhydrase; kidney concentrating mechanism.
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|---|---|
| ln Vitro |
In isolated perfused rat liver, mefruside (0.3 mM; 50 minutes) reduces urea production by 34% [1]. In isolated perfused rat liver, mefruside (0.25, 0.5, 0.75, 1, 1.25 mM) suppresses urea production in a concentration-dependent manner [1]. Determination of cell viability [1]
Mefruside inhibits carbonic anhydrase activity, leading to increased sodium chloride excretion. It affects the kidney's concentrating function. The compound inhibits urea synthesis in an isolated rat liver perfusion model. It may not spare potassium, distinguishing it from potassium-sparing diuretics. |
| ln Vivo |
Mefruside has diuretic and mild antihypertensive effects in vivo. The peak effect occurs at 6-12 hours and duration is 20-24 hours. It causes less potassium excretion compared to hydrochlorothiazide. The compound is used to treat edema and hypertension. It increases sodium chloride excretion and may increase blood uric acid levels.
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| Enzyme Assay |
In vitro enzyme assays measure carbonic anhydrase inhibition. Purified carbonic anhydrase is incubated with p-nitrophenyl acetate substrate and varying concentrations of Mefruside (typically 0.1-100 µM). Enzyme activity is measured spectrophotometrically at 348 nm. IC50 values are calculated from dose-response curves. Selectivity is assessed against different carbonic anhydrase isoforms. Urea synthesis inhibition is measured in isolated perfused rat liver models.
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| Cell Assay |
Cell viability determination [1]
Cell Types: Rat liver (male Wistar rats weighing 120-220 g; isolated perfusion model) Tested Concentrations: 0.3 mM Incubation Duration: 50 min Experimental Results: The inhibition rate of urea synthesis was 34%. In vitro cellular assays are performed using kidney epithelial cell lines (e.g., MDCK or LLC-PK1 cells). Cells are treated with Mefruside at concentrations ranging from 0.1-100 µM for 24-48 hours. Ion transport is assessed by measuring sodium and chloride flux using ion-selective electrodes or fluorescent dyes. Cell viability is monitored using MTT assays. Carbonic anhydrase activity in cell lysates is measured using a CO2 hydration assay. |
| Animal Protocol |
In vivo efficacy is evaluated in rat or dog models of diuresis. Mefruside is administered orally at doses ranging from 1-20 mg/kg. Urine volume, sodium, potassium, and chloride excretion are measured over 24 hours. Blood pressure is monitored in hypertensive animal models. Uric acid levels are measured in serum. For urea synthesis studies, isolated perfused rat liver models are used with compound administration.
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| ADME/Pharmacokinetics |
Mefruside has a molecular weight of 382.9 g/mol and molecular formula C13H19ClN2O5S2. CAS number: 7195-27-9. It is orally bioactive. Store as a powder at room temperature. Soluble in DMSO and organic solvents. The compound is stable under normal storage conditions. For in vivo use, formulate in suitable vehicle for oral administration.
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| Toxicity/Toxicokinetics |
Mefruside is generally well-tolerated at therapeutic doses. Side effects may include electrolyte imbalances, increased uric acid levels, and gastrointestinal disturbances. As a diuretic, it may cause hypokalemia. Contraindications include severe renal impairment and hypersensitivity to sulfonamides. The compound is for research use only and not for human therapeutic use outside of approved indications.
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| References | |
| Additional Infomation |
Mefruside is an organic molecular entity belonging to the benzenesulfonamide furan class of compounds. Used as a diuretic, it affects the kidney's concentrating function, increasing sodium chloride excretion but potentially not retaining potassium. It inhibits carbonic anhydrase and may raise uric acid levels in the blood.
Mefruside is a diuretic agent developed by Bayer A.G.. It is used for the treatment of edema and hypertension. The compound is also known as Baycaron. It is a benzene-sulfonamide-furan derivative. Mefruside is supplied as a research compound with high purity and should be stored at room temperature. It is a valuable tool for studying renal physiology and diuretic mechanisms. |
| Molecular Formula |
C13H19CLN2O5S2
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|---|---|
| Molecular Weight |
382.874
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| Exact Mass |
382.042
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| CAS # |
7195-27-9
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| Related CAS # |
Mefruside-d3;2468638-25-5
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| PubChem CID |
4047
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| Appearance |
White to off-white solid powder
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| Density |
1.417g/cm3
|
| Boiling Point |
565.2ºC at 760 mmHg
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| Melting Point |
149.5°C
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| Flash Point |
295.6ºC
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| Index of Refraction |
1.571
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| LogP |
4.038
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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 |
5
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| Heavy Atom Count |
23
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| Complexity |
628
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(S(N(CC2(CCCO2)C)C)(=O)=O)=CC=1S(=O)(N)=O
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| InChi Key |
SMNOERSLNYGGOU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H19ClN2O5S2/c1-13(6-3-7-21-13)9-16(2)23(19,20)10-4-5-11(14)12(8-10)22(15,17)18/h4-5,8H,3,6-7,9H2,1-2H3,(H2,15,17,18)
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| Chemical Name |
4-chloro-1-N-methyl-1-N-[(2-methyloxolan-2-yl)methyl]benzene-1,3-disulfonamide
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| Synonyms |
FDA 1902; FDA-1902; FDA1902
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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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.6119 mL | 13.0593 mL | 26.1185 mL | |
| 5 mM | 0.5224 mL | 2.6119 mL | 5.2237 mL | |
| 10 mM | 0.2612 mL | 1.3059 mL | 2.6119 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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