| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Sulfisomidine targets the bacterial enzyme dihydropteroate synthase (DHPS), similar to other sulfonamides. As a structural analogue of para-aminobenzoic acid (PABA), it acts as a competitive inhibitor of DHPS, blocking the synthesis of folic acid. This inhibition disrupts the production of tetrahydrofolate, which is essential for the synthesis of nucleic acids and proteins in bacteria. The compound has broad-spectrum activity against Gram-positive and Gram-negative organisms.
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| ln Vitro |
Sulfaisodimidine (Sulfaisodimidine) is an antibacterial agent with a short half-life [1].
Sulfisomidine demonstrates broad-spectrum antibacterial activity against a variety of Gram-positive and Gram-negative organisms. It is effective against infections caused by susceptible bacteria, including urinary tract infections, respiratory infections, and gastrointestinal infections. The compound's bacteriostatic effect is due to its ability to inhibit folic acid synthesis. It is used as a biochemical tool in studies of microbial metabolism and enzyme inhibition. |
| ln Vivo |
Sulfisomidine is an orally active short-acting sulfonamide antibacterial. It was investigated in the 1950s for the treatment of urinary tract infections. It is effective against a variety of infections, including urinary tract infections, respiratory infections, and gastrointestinal infections. It is currently unclear whether sulfisomidine has received formal approval in any region. It is primarily used as a biochemical tool in research.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for sulfisomidine typically involve evaluating its inhibitory activity against dihydropteroate synthase (DHPS). The enzyme is incubated with varying concentrations of sulfisomidine and a fixed concentration of para-aminobenzoic acid (PABA). The reaction is monitored by measuring the formation of dihydrofolate, and the IC50 is determined.
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| Cell Assay |
For in vitro cell-based assays, sulfisomidine is dissolved in DMSO (50 mg/mL; 179.64 mM) and applied to cultured bacterial cells at concentrations ranging from 1-100 µg/mL. The Minimum Inhibitory Concentration (MIC) is determined using standard broth dilution methods.
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| Animal Protocol |
In vivo animal studies for sulfisomidine are typically conducted in rodent models of bacterial infection. The compound is administered orally at doses ranging from 10-100 mg/kg. Efficacy is evaluated by measuring bacterial load in tissues and clinical signs of infection.
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| ADME/Pharmacokinetics |
Sulfisomidine has a molecular weight of 278.33 g/mol and a molecular formula of C12H14N4O2S. It is soluble in DMSO (50 mg/mL; 179.64 mM) and freely soluble in dilute HCl and NaOH, but practically insoluble in benzene, ether, and chloroform. The compound is typically stored as a powder at -20°C for long-term stability. Sulfisomidine is also known as sulfaisodimidine. It has the SMILES O=S(C1=CC=C(N)C=C1)(NC2=NC(C)=NC(C)=C2)=O.
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| Toxicity/Toxicokinetics |
Sulfisomidine is considered to have a manageable toxicity profile consistent with other sulfonamide antibiotics. Common adverse effects include hypersensitivity reactions, such as skin rashes. Hematological toxicities, including agranulocytosis and hemolytic anemia, can occur. Renal toxicity, such as crystalluria, is a risk. Gastrointestinal disturbances, including nausea and vomiting, are also reported.
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| References | |
| Additional Infomation |
Sulfisomidine is a sulfonamide drug composed of a pyrimidine ring with methyl substituents at positions 2 and 6 and a 4-aminobenzenesulfonamide group at position 4. It is an anti-infective drug. It belongs to the pyrimidine, sulfonamide, and sulfonamide antibiotic classes. Its function is related to sulfonamide drugs. Sulfisomidine (also known as sulfadiazine) is an antibacterial drug that was investigated in the 1950s for the treatment of urinary tract infections, but it is currently unclear whether this drug has received formal approval in any region. A sulfonamide antibacterial drug. See also: Sulfamethazine (note moved to).
Sulfisomidine is a short-acting sulfonamide antibacterial compound. It is a sulfanilamide antibacterial agent used as a biochemical tool in studies of microbial metabolism and enzyme inhibition. Sulfisomidine was investigated in the 1950s for the treatment of urinary tract infections. It is an orally active short-acting sulfonamide antibacterial. It has broad-spectrum activity against Gram-positive and Gram-negative organisms. It is currently unclear whether sulfisomidine has received formal approval in any region. |
| Molecular Formula |
C12H14N4O2S
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|---|---|
| Molecular Weight |
278.33016
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| Exact Mass |
278.083
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| CAS # |
515-64-0
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| PubChem CID |
5343
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
480.7±55.0 °C at 760 mmHg
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| Melting Point |
245ºC
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| Flash Point |
244.5±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.644
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| LogP |
-0.43
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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 |
3
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| Heavy Atom Count |
19
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| Complexity |
387
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C1=CC=C(N)C=C1)(NC2=NC(C)=NC(C)=C2)=O
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| InChi Key |
YZMCKZRAOLZXAZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H14N4O2S/c1-8-7-12(15-9(2)14-8)16-19(17,18)11-5-3-10(13)4-6-11/h3-7H,13H2,1-2H3,(H,14,15,16)
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| Chemical Name |
4-amino-N-(2,6-dimethylpyrimidin-4-yl)benzenesulfonamide
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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 : ~100 mg/mL (~359.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.98 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 25.0 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: ≥ 2.5 mg/mL (8.98 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5929 mL | 17.9643 mL | 35.9286 mL | |
| 5 mM | 0.7186 mL | 3.5929 mL | 7.1857 mL | |
| 10 mM | 0.3593 mL | 1.7964 mL | 3.5929 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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