| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g |
|
||
| 5g |
|
||
| Other Sizes |
|
| ln Vitro |
The nature of sulfamethazine is bacteriostatic. Bacterial nucleotide and DNA synthesis is decreased when dihydrofolate production is inhibited [1].
|
|---|---|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed following oral administration. Metabolism / Metabolites Sulfamerazine has known human metabolites that include N(4)-Acetylsulfamerazine. |
| References | |
| Additional Infomation |
Sulfamerazine is a sulfonamide consisting of pyrimidine with a methyl substituent at the 4-position and a 4-aminobenzenesulfonamido group at the 2-position. It has a role as an antiinfective agent and a drug allergen. It is a member of pyrimidines, a sulfonamide and a sulfonamide antibiotic. It is functionally related to a sulfanilamide.
A sulfanilamide that is used as an antibacterial agent. Sulfamerazine is a long-acting sulfanilamide antibacterial agent. Sulfamerazine inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for the binding site on dihydropteroate synthase. A sulfanilamide that is used as an antibacterial agent. See also: Sulfamerazine Sodium (is active moiety of); Sulfadiazine; sulfamerazine (component of); Sulfamerazine; Sulfamethazine; Sulfaquinoxaline (component of). Drug Indication A sulfanilamide that is used as an antibacterial agent. It can be used to treat bronchitis, prostatitis and urinary tract infections. Mechanism of Action Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase). Sulfamerazine is bacteriostatic in nature. Inhibition of dihydrofolic acid synthesis decreases the synthesis of bacterial nucleotides and DNA. Pharmacodynamics Sulfonamides act as competitive inhibitors of the enzyme dihydropteroate synthetase (DHPS), an enzyme involved in folate synthesis in bacteria. |
| 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
