| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g |
|
||
| 5g |
|
||
| Other Sizes |
| Targets |
Sulfamerazine targets bacterial dihydropteroate synthase (DHPS). By competitively inhibiting DHPS, it blocks the synthesis of folic acid, which is essential for bacterial growth and replication. This mechanism is the basis for its antibacterial activity.
|
|---|---|
| ln Vitro |
The nature of sulfamethazine is bacteriostatic. Bacterial nucleotide and DNA synthesis is decreased when dihydrofolate production is inhibited [1].
In vitro, sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid. It is effective against a variety of bacteria. Its antibacterial activity is well-characterized. |
| ln Vivo |
In vivo, sulfamerazine is used as an antibiotic for the treatment of various bacterial infections. It has higher efficacy against infections caused by hemolytic streptococci and pneumococci compared to sulfadiazine. It is administered orally or parenterally.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for sulfamerazine typically involve evaluating its inhibitory activity against purified DHPS. The enzyme is incubated with varying concentrations of sulfamerazine and its substrate, para-aminobenzoic acid (PABA). The reaction is monitored by measuring the formation of dihydrofolate, and the IC₅₀ is determined.
|
| Cell Assay |
For in vitro cell-based assays, sulfamerazine is dissolved in DMSO or aqueous buffers 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. The effects on bacterial growth are assessed.
|
| Animal Protocol |
In vivo animal studies for sulfamerazine are typically conducted in rodent models of bacterial infection. Sulfamerazine is administered orally or parenterally at doses ranging from 10-100 mg/kg. Efficacy is evaluated by measuring bacterial load, clinical signs, and survival.
|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed after oral administration. Metabolism/Metabolites Known human metabolites of sulfadiazine include N(4)-acetylsulfadiazine. Sulfamerazine has a molecular formula of C₁₁H₁₂N₄O₂S and a molecular weight of 264.30 g/mol. It is a white to off-white crystalline powder. It is slightly soluble in water and ethanol, but soluble in dilute mineral acids and alkaline solutions. |
| Toxicity/Toxicokinetics |
Sulfamerazine is considered to have a manageable toxicity profile. As a sulfonamide, it may cause hypersensitivity reactions, hematological toxicities, and renal toxicity. Appropriate safety precautions should be followed when handling the compound.
|
| References | |
| Additional Infomation |
Sulfadiazine is a sulfonamide compound composed of a pyrimidine ring with a methyl substituent at position 4 and a 4-aminobenzenesulfonamide group at position 2. It has anti-infective and anti-drug allergen effects. It belongs to the pyrimidine, sulfonamide, and sulfonamide antibiotic classes. Its function is related to sulfonamide compounds. Sulfonamide compounds are sulfonamide drugs used as antibacterial agents. Sulfadiazine is a long-acting sulfonamide antibacterial agent. Sulfadiazine inhibits bacterial synthesis of dihydrofolate by competing with para-aminobenzoic acid (PABA) for binding sites on dihydropteroate synthase. See also: sulfadiazine sodium (its active moiety); sulfadiazine; sulfadiazine (ingredient); sulfadiazine; Sulfadimethoxine; sulfaquinoxaline (ingredient).
Drug Indications Sulfadiazine is a sulfonamide drug used as an antibacterial agent. It can be used to treat bronchitis, prostatitis, and urinary tract infections. Mechanism of Action Sulfadiazine is a sulfonamide drug that inhibits bacterial dihydrofolate synthesis by competitively binding to dihydropteroate synthase (DHPS), an enzyme involved in bacterial folate synthesis. Sulfadiazine has antibacterial activity. Inhibition of dihydrofolate synthesis reduces bacterial nucleotide and DNA synthesis. Pharmacodynamics Sulfonamide drugs act as competitive inhibitors of dihydropteroate synthase (DHPS), an enzyme involved in bacterial folate synthesis. Sulfamerazine is a sulfonamide antibiotic used for the treatment of various bacterial infections. It is also known as sulphamerazine. Sulfamerazine is approved for clinical use in some countries. It is supplied by various pharmaceutical and research chemical suppliers for human and research use. |
| Molecular Formula |
C11H12N4O2S
|
|---|---|
| Molecular Weight |
264.303
|
| Exact Mass |
264.068
|
| CAS # |
127-79-7
|
| Related CAS # |
Sulfamerazine sodium salt;127-58-2;Sulfamerazine-d4;1020719-84-9
|
| PubChem CID |
5325
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
519.1±52.0 °C at 760 mmHg
|
| Melting Point |
234-238°C
|
| Flash Point |
267.8±30.7 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.660
|
| LogP |
0.34
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
18
|
| Complexity |
360
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])N([H])[H])(N([H])C1=NC([H])=C([H])C(C([H])([H])[H])=N1)(=O)=O
|
| InChi Key |
QPPBRPIAZZHUNT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H12N4O2S/c1-8-6-7-13-11(14-8)15-18(16,17)10-4-2-9(12)3-5-10/h2-7H,12H2,1H3,(H,13,14,15)
|
| Chemical Name |
4-amino-N-(4-methylpyrimidin-2-yl)benzenesulfonamide
|
| Synonyms |
Methylsulfadiazine; Mebacid; Sulfamerazine
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
DMSO : ≥ 100 mg/mL (~378.36 mM)
H2O : ~0.1 mg/mL (~0.38 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.46 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 (9.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7836 mL | 18.9179 mL | 37.8358 mL | |
| 5 mM | 0.7567 mL | 3.7836 mL | 7.5672 mL | |
| 10 mM | 0.3784 mL | 1.8918 mL | 3.7836 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
