| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
Mafenide hydrochloride targets bacterial infections with a broad spectrum of activity. Its primary mechanism involves inhibiting nucleotide synthesis in both Gram-positive and Gram-negative organisms. Additionally, it inhibits the enzyme carbonic anhydrase. Other reported targets include tau fibril formation and human tyrosyl-DNA phosphodiesterase 1 (TDP1).
|
|---|---|
| ln Vitro |
Mafenide hydrochloride demonstrates broad-spectrum antibacterial activity against Gram-positive and Gram-negative organisms, including Pseudomonas aeruginosa. It inhibits nucleotide synthesis in susceptible bacteria. Additional in vitro activities include inhibition of tau fibril formation, induction of DNA re-replication in SW480 colon adenocarcinoma cells, and inhibition of human tyrosyl-DNA phosphodiesterase 1 (TDP1).
|
| ln Vivo |
In vivo, mafenide hydrochloride is effective as a topical anti-infective agent for burn wounds. It prevents bacterial colonization and infection in damaged tissue. The compound is applied topically and shows activity against a range of pathogens commonly found in burn wounds. Its clinical utility is well established in burn therapy.
|
| Enzyme Assay |
A typical non-cellular enzyme/receptor binding assay for mafenide involves testing its inhibition of carbonic anhydrase. The enzyme is incubated with varying concentrations of the compound in a suitable buffer. The reaction is initiated by adding a substrate, and enzyme activity is measured spectrophotometrically by monitoring product formation or substrate depletion. IC₅₀ values are calculated from dose-response curves.
|
| Cell Assay |
For in vitro antibacterial activity testing, bacterial strains are cultured in appropriate media to logarithmic phase. Bacterial suspensions are adjusted to a standard density (e.g., 1×10⁶ CFU/mL) and added to 96-well plates containing serial dilutions of mafenide hydrochloride. Plates are incubated at 35°C for 18-24 hours. The minimum inhibitory concentration (MIC) is determined as the lowest concentration that completely inhibits visible bacterial growth.
|
| Animal Protocol |
In vivo efficacy is typically evaluated in animal models of burn wound infection. Mice or rats are subjected to partial-thickness burn wounds, which are then infected with a bacterial pathogen such as Pseudomonas aeruginosa. The test compound is applied topically to the wound site, and the extent of bacterial colonization, wound healing, and survival are monitored over several days. Efficacy is compared to vehicle-treated and untreated control groups.
|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following topical application, mafenib can be absorbed into the systemic circulation through areas with poor vascular distribution. Renal Metabolites: Metabolites are rapidly excreted in high concentrations in the urine; however, the parent compound has not been detected in urine. Metabolism/Metabolites Metabolized to a carbonic anhydrase inhibitor. Mafenide hydrochloride is administered topically, resulting in local absorption. Systemic absorption through burn wounds can occur but is generally limited. The compound is metabolized and excreted primarily via the kidneys. Its half-life and systemic exposure depend on the extent of the wound and the dosage form used. Detailed PK parameters in humans are limited as it is primarily used as a topical agent. |
| Toxicity/Toxicokinetics |
Mafenide hydrochloride is generally well-tolerated when used topically. Local side effects may include burning, stinging, or rash. Systemic toxicity is uncommon but can occur with extensive application over large burn wounds. Potential adverse effects include metabolic acidosis due to carbonic anhydrase inhibition. The compound is for research and topical use only; systemic use is not recommended.
|
| Additional Infomation |
Sulfamilone is an aromatic amine. Sulfamilone is a sulfonamide antibacterial agent used to treat severe burns. It promotes healing of deep burns by reducing the number of bacteria in burned tissue. In 1998, sulfamilone acetate was approved under the FDA's accelerated approval program. In November 2022, the FDA withdrew the approval of sulfamilone acetate (5% topical solution powder) because an incomplete confirmatory study failed to meet the requirements for accelerated approval. Sulfamilone is a methylated sulfonamide antibacterial agent. It is a sulfonamide drug that inhibits carbonic anhydrase and is used as a topical antibacterial agent, particularly for the treatment of burns. See also: Sulfamilone acetate (in salt form). Mafenib hydrochloride (in salt form).
Drug Indications Indicated as an adjunct topical antibacterial agent to control bacterial infection when covering a wet dressing on an autologous mesh graft after excision of a burn wound. FDA Label Mechanism of Action The exact mechanism of action of masfennig is not yet clear. However, masfennig can reduce the number of bacteria in avascular burn tissue and promote the self-healing of deep burns. Mafenide hydrochloride is a sulfonamide antimicrobial first introduced for burn wound management. It is available as a topical cream or solution. The compound's antibacterial mechanism involves inhibition of nucleotide synthesis, distinguishing it from other sulfonamides that primarily inhibit folate synthesis. It remains clinically relevant for treating burn wound infections, particularly those caused by Pseudomonas aeruginosa. This product is for research purposes only and not for human therapeutic use. |
| Molecular Formula |
C7H11CLN2O2S
|
|---|---|
| Molecular Weight |
222.6924
|
| Exact Mass |
222.022
|
| CAS # |
138-37-4
|
| Related CAS # |
Mafenide Acetate;13009-99-9;Mafenide;138-39-6
|
| PubChem CID |
3998
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
382ºC at 760mmHg
|
| Melting Point |
261-263 °C(lit.)
|
| Flash Point |
184.8ºC
|
| LogP |
3.076
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
12
|
| Complexity |
224
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl[H].S(C1C([H])=C([H])C(C([H])([H])N([H])[H])=C([H])C=1[H])(N([H])[H])(=O)=O
|
| InChi Key |
TYMRLRRVMHJFTF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C7H10N2O2S/c8-5-6-1-3-7(4-2-6)12(9,10)11/h1-4H,5,8H2,(H2,9,10,11)
|
| Chemical Name |
4-(aminomethyl)benzenesulfonamide
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~125 mg/mL (~561.32 mM)
|
|---|---|
| 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 | 4.4905 mL | 22.4527 mL | 44.9055 mL | |
| 5 mM | 0.8981 mL | 4.4905 mL | 8.9811 mL | |
| 10 mM | 0.4491 mL | 2.2453 mL | 4.4905 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
