| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target is bacterial dihydropteroate synthase (DHPS), an enzyme in the folate biosynthesis pathway. DHPS catalyzes the condensation of para-aminobenzoic acid (PABA) with dihydropteroate diphosphate to form dihydropteroate, a precursor of tetrahydrofolate. Sulfamerazine acts as a competitive antagonist of PABA, inhibiting DHPS and blocking folate synthesis. This leads to inhibition of bacterial growth and replication.
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|---|---|
| ln Vitro |
In vitro, Sulfamerazine sodium salt exhibits antibacterial activity against a range of gram-positive and gram-negative bacteria, including Escherichia coli, Staphylococcus aureus, and Streptococcus pneumoniae, with MIC values typically in the range of 1-64 µg/mL. It is bacteriostatic and requires the presence of PABA-free medium for optimal activity. The compound is used as a reference sulfonamide in antibacterial susceptibility testing.
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| ln Vivo |
In vivo, Sulfamerazine sodium salt is effective in treating bacterial infections in animal models. It is administered intravenously or intramuscularly for systemic infections and orally for gastrointestinal infections. It is often used in combination with trimethoprim (co-trimazine) for synergistic antibacterial activity. However, its clinical use has declined due to the emergence of sulfonamide-resistant bacteria.
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| Enzyme Assay |
For non-cellular enzyme assays, bacterial dihydropteroate synthase is incubated with dihydropteroate diphosphate and [14C]-PABA in assay buffer. Serial dilutions of Sulfamerazine sodium salt are added, and the reaction is incubated at 37°C. The reaction is terminated, and product formation is quantified by scintillation counting or HPLC. IC50 values are determined from dose-response curves.
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| Cell Assay |
For cell-based assays, bacterial cultures are grown in Mueller-Hinton broth and treated with serial dilutions of Sulfamerazine sodium salt in 96-well plates. After 18-24 hours of incubation at 37°C, bacterial growth is assessed by measuring optical density at 600 nm. The MIC is defined as the lowest concentration that inhibits visible growth. Checkerboard assays are used to assess synergy with trimethoprim.
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| Animal Protocol |
For in vivo experiments, mice are infected with a lethal dose of bacteria (e.g., E. coli, S. aureus) via intraperitoneal or intravenous injection. Sulfamerazine sodium salt is administered intravenously or intramuscularly at various doses (e.g., 10-100 mg/kg) starting at 1 hour post-infection. Animal survival is monitored for 5-7 days, and bacterial burden in blood and organs is quantified by CFU counting.
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| References | |
| Additional Infomation |
Sulfamethazine sodium is a sulfonamide drug. Sulfamethazine sodium is the sodium salt form of sulfamethazine, a long-acting sulfonamide antibacterial agent. See also: ... View more ...
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| Molecular Formula |
C11H11N4NAO2S
|
|---|---|
| Molecular Weight |
286.28
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| Exact Mass |
286.05
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| CAS # |
127-58-2
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| Related CAS # |
Sulfamerazine;127-79-7;Sulfamerazine-d4;1020719-84-9
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| PubChem CID |
15899899
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
519.1ºC at 760mmHg
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| Melting Point |
216-219 °C
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| Flash Point |
267.8ºC
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| Vapour Pressure |
7.03E-11mmHg at 25°C
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| LogP |
2.688
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| Hydrogen Bond Donor Count |
1
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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 |
365
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S([N-]C1=NC=CC(C)=N1)(C2=CC=C(N)C=C2)=O.[Na+]
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| InChi Key |
BSFJGCCAXDCMOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H11N4O2S.Na/c1-8-6-7-13-11(14-8)15-18(16,17)10-4-2-9(12)3-5-10;/h2-7H,12H2,1H3;/q-1;+1
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| Chemical Name |
sodium;(4-aminophenyl)sulfonyl-(4-methylpyrimidin-2-yl)azanide
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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) |
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 | 3.4931 mL | 17.4654 mL | 34.9308 mL | |
| 5 mM | 0.6986 mL | 3.4931 mL | 6.9862 mL | |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.4931 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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