| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| 50g |
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| Other Sizes |
| Targets |
Acriflavine targets nucleic acids (DNA and RNA). Its mechanism of action involves intercalation, where it inserts itself between the base pairs of the DNA double helix. This intercalation disrupts the structure of the DNA, interfering with replication and transcription processes. This inhibition of nucleic acid synthesis is the basis for its antibacterial and antiviral activity. It is also used as a fluorescent probe to label high molecular weight RNA.
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| ln Vitro |
It was discovered that acrylavine is a powerful MCT4 dye that inhibits the binding of basigin to MCT4. Numerous astroblastoma neurosphere cell lines exhibit considerable growth and self-renewal inhibition when exposed to acrylamide [1]. Acriflavine, which inhibits the matrix and CML cell proliferation, is equivalent to HIF-1. It may reduce CML cells' capacity to produce stem cells [2].
In vitro, Acriflavine is a fluorescent dye used for labeling high molecular weight RNA. It has antibacterial and antiviral activity due to its ability to intercalate into nucleic acids. Its antimicrobial activity is assessed by measuring its ability to inhibit the growth of bacteria and viruses in culture. Quantitative MIC values are not detailed in the publicly available sources. |
| ln Vivo |
Acriflavine has the ability to prevent VEGF expression and the development of blood vessels in tumors [1]. Acriflavine inhibited the growth of animal models and the upkeep of LSCs in mouse tumor CML models [2]. In mouse tumor models, acriflavine slows the growth of tumors. When sunitinib and arciflavine are taken together, there is a considerable reduction in the expression of TGF-β and vascular endothelial growth factor, as well as a reduction in tumor blood vessels. This leads to an increase in tumor medial wall and cell inflammation [3].
In vivo, Acriflavine is used as a topical antiseptic for the treatment of infected wounds and for skin disinfection. It is applied topically to the affected area. Its effectiveness is based on its ability to inhibit the growth of microorganisms at the site of application. It is not used systemically due to its toxicity. |
| Enzyme Assay |
For in vitro cell-free assays, the interaction of Acriflavine with nucleic acids can be studied using spectrophotometric or fluorometric methods. The binding of Acriflavine to DNA or RNA results in changes in its absorption and fluorescence spectra. These changes can be used to measure the binding affinity and stoichiometry of the interaction. Its ability to intercalate can also be studied using DNA unwinding assays or gel mobility shift assays.
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| Cell Assay |
For in vitro cellular assays, the antibacterial and antiviral activity of Acriflavine is assessed in cell culture. Bacteria or viruses are cultured in the presence of varying concentrations of the compound, and the inhibition of growth or replication is measured. Its cytotoxicity can be assessed in mammalian cell lines to determine its selectivity.
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| Animal Protocol |
In vivo, the efficacy of Acriflavine as a topical antiseptic is evaluated in animal models of wound infection or in clinical use. The compound is applied topically to infected wounds, and the reduction in bacterial load and improvement in wound healing are assessed.
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| ADME/Pharmacokinetics |
Acriflavine has a molecular formula of C14H14ClN3 and a molecular weight of 259.73 g/mol. Its CAS number is 8048-52-0. It is a fluorescent dye and is typically supplied as a powder. It is soluble in water and ethanol. For in vitro studies, stock solutions are prepared in water or ethanol. For topical application, it is formulated in suitable vehicles. Storage is recommended at room temperature, protected from light. Its purity is typically >98% for research use.
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| Toxicity/Toxicokinetics |
Acriflavine has moderate toxicity. It is used only as a topical agent due to its systemic toxicity. It can cause skin irritation and staining. Its use has declined due to the availability of safer and more effective antiseptics.
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| References |
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| Additional Infomation |
A mixture of 3,6-diamino-10-methylacridinium chloride and 3,6-acridinium diamine. A fluorescent dye used as a topical disinfectant and biological staining agent. It can intercalate into nucleic acids, thereby inhibiting the replication of bacteria and viruses.
See also: Acridine Yellow (note moved to). Acriflavine is an approved topical antiseptic in some countries, though its use is limited. It is not FDA-approved for systemic use. Its mechanism of action involves the intercalation into nucleic acids, inhibiting bacterial and viral replication. It is also used as a biological stain and fluorescent probe. |
| Molecular Formula |
C14H14N3.CL.C13H11N3
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|---|---|
| Molecular Weight |
468.9895
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| Exact Mass |
468.182
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| CAS # |
8048-52-0
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| Related CAS # |
Acriflavine hydrochloride;69235-50-3
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| PubChem CID |
443101
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| Appearance |
Light brown to brown solid powder
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| Melting Point |
179-181 °C
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| LogP |
3.863
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
34
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| Complexity |
486
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[N+]1=C2C=C(C=CC2=CC3=C1C=C(C=C3)N)N.C1=CC(=CC2=NC3=C(C=CC(=C3)N)C=C21)N.[Cl-]
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| InChi Key |
PEJLNXHANOHNSU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H13N3.C13H11N3.ClH/c1-17-13-7-11(15)4-2-9(13)6-10-3-5-12(16)8-14(10)17;14-10-3-1-8-5-9-2-4-11(15)7-13(9)16-12(8)6-10;/h2-8H,1H3,(H3,15,16);1-7H,14-15H2;1H
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| Chemical Name |
acridine-3,6-diamine;10-methylacridin-10-ium-3,6-diamine;chloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : ≥ 25 mg/mL (~96.25 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (7.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1322 mL | 10.6612 mL | 21.3224 mL | |
| 5 mM | 0.4264 mL | 2.1322 mL | 4.2645 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1322 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.
Link: https://clinicaltrials.gov/ct2/show/NCT03379389
Conditions:Urinary Tract InfectionsProducts are for research use only; We do not sell to patients
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