| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Proflavine dihydrochloride targets bacterial DNA. As a DNA intercalating agent, it binds to double-stranded DNA by inserting between adjacent base pairs. This intercalation disrupts the normal helical structure of DNA, inhibiting both replication and transcription. The inhibition of DNA synthesis prevents bacterial cell division, leading to a bacteriostatic effect. Its selectivity for bacterial DNA over mammalian DNA is limited, which restricts its systemic use. It is primarily used as a topical antiseptic.
|
|---|---|
| ln Vitro |
In vitro, Proflavine dihydrochloride exhibits antimicrobial activity against a range of bacteria. Its activity is assessed by determining the minimum inhibitory concentration (MIC) against various bacterial strains using standard broth microdilution or agar diffusion methods. As a DNA intercalator, it inhibits DNA synthesis, which can be measured by assessing the incorporation of radiolabeled thymidine into bacterial DNA. Its cytotoxicity to mammalian cells is also assessed in vitro, as it intercalates into DNA regardless of the source.
|
| ln Vivo |
Detailed in vivo activity data for Proflavine dihydrochloride are not extensively provided in the search results. As a topical antiseptic, it is applied to wounds or mucous membranes to prevent or treat infections. Its systemic use is limited due to its toxicity. In animal models of wound infection, it would be expected to reduce bacterial load. Its in vivo efficacy is influenced by its ability to penetrate tissues and its interaction with serum proteins. Its use has declined with the introduction of safer and more effective antiseptics.
|
| Enzyme Assay |
In vitro antimicrobial susceptibility testing is performed using standard methods such as the broth microdilution or agar dilution method according to CLSI guidelines. Bacterial cultures are grown overnight and diluted to a standard inoculum. Serial two-fold dilutions of Proflavine dihydrochloride are prepared in 96-well microtiter plates. Each well is inoculated with bacterial suspension and incubated at 37°C for 18-24 hours. The MIC is defined as the lowest concentration that inhibits visible bacterial growth.
|
| Cell Assay |
For in vitro cell-based assays, bacterial cells or mammalian cell lines can be used. For DNA synthesis inhibition, bacterial cells are treated with Proflavine dihydrochloride and [³H]thymidine. The incorporation of radioactivity into DNA is measured. For cytotoxicity, mammalian cells are treated with serial dilutions of the compound, and cell viability is assessed using MTT or other assays. The IC50 for cytotoxicity is calculated and compared to the MIC to determine the selectivity index.
|
| Animal Protocol |
In vivo animal studies for topical antiseptic efficacy are conducted in wound infection models in rodents. A wound is created on the animal's skin, and a bacterial inoculum is applied. Proflavine dihydrochloride is applied topically, and the bacterial burden in the wound is measured by taking biopsies and performing bacterial counts. The reduction in bacterial load compared to untreated controls is assessed. Skin irritation and sensitization studies are also conducted to evaluate local tolerability.
|
| References |
|
| Additional Infomation |
Proflavine dihydrochloride is an orange-red to brownish-red Crystals powder. Its pH (0.1% aqueous solution) is 2.5-3.0. 3,6-Diaminoacridine dihydrochloride is a hydrochloride formed by the reaction of 3,6-diaminoacridine with 2 molar equivalents of hydrogen chloride. It has antibacterial, preservative, carcinogenic, and intercalating agent properties. It contains 3,6-diaminoacridine(2+) ions.
|
| Molecular Formula |
C13H13CL2N3
|
|---|---|
| Molecular Weight |
282.17
|
| Exact Mass |
281.049
|
| CAS # |
531-73-7
|
| Related CAS # |
Proflavine hemisulfate;1811-28-5
|
| PubChem CID |
10750
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
506.9ºC at 760mmHg
|
| Flash Point |
292.9ºC
|
| LogP |
5.318
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
18
|
| Complexity |
232
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=CC2=NC3=C(C=CC(=C3)N)C=C12)N.Cl.Cl
|
| InChi Key |
YHIHFKAEJAVELI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H11N3.2ClH/c14-10-3-1-8-5-9-2-4-11(15)7-13(9)16-12(8)6-10;;/h1-7H,14-15H2;2*1H
|
| Chemical Name |
acridine-3,6-diamine;dihydrochloride
|
| Synonyms |
Proflavine HCl; Proflavine dihydrochloride
|
| 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) |
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
|
|---|---|
| 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 | 3.5440 mL | 17.7198 mL | 35.4396 mL | |
| 5 mM | 0.7088 mL | 3.5440 mL | 7.0879 mL | |
| 10 mM | 0.3544 mL | 1.7720 mL | 3.5440 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
