| Targets |
Acriflavine hydrochloride targets papain-like protease (PLpro) of SARS-CoV-2. PLpro is a viral protease essential for viral replication and immune evasion. By inhibiting PLpro, Acriflavine hydrochloride blocks SARS-CoV-2 replication. It also has antimicrobial and antiseptic properties, and is used in cancer research.
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|---|---|
| ln Vitro |
In vitro, Acriflavine hydrochloride is a potent inhibitor of SARS-CoV-2 PLpro. It has antimicrobial, antifungal, and antiparasitic activities. It is used in cancer research, including breast cancer, brain tumor, and chronic myeloid leukemia. Acriflavine hydrochloride is a mixture of proflavine and trypaflavine.
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| ln Vivo |
In vivo data for Acriflavine hydrochloride is not extensively reported in publicly available sources. As an antiseptic, it has been used topically for wound disinfection. As a PLpro inhibitor, it has potential applications in animal models of SARS-CoV-2 infection. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro PLpro inhibition assay for Acriflavine hydrochloride uses recombinant SARS-CoV-2 PLpro enzyme and a fluorogenic peptide substrate. Enzyme activity is measured by monitoring the cleavage of the substrate, and IC50 values are calculated from dose-response curves. Antimicrobial activity is assessed using standard broth microdilution methods to determine minimum inhibitory concentrations (MICs).
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| Cell Assay |
Cellular assays for Acriflavine hydrochloride are conducted in virus-infected cells and cancer cell lines. For antiviral studies, cells are infected with SARS-CoV-2 and treated with varying concentrations of Acriflavine hydrochloride. Viral replication is measured by quantifying viral RNA or by plaque assay. For cancer studies, cell viability and proliferation are measured using standard assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo studies for Acriflavine hydrochloride would typically involve animal models of SARS-CoV-2 infection or cancer. The compound would be administered via oral, intraperitoneal, or topical routes. Efficacy would be assessed by measuring viral loads, tumor growth, or wound healing. However, specific published in vivo protocols for Acriflavine hydrochloride are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Acriflavine hydrochloride is not extensively reported. The compound has a molecular weight of 541.90 g/mol and a molecular formula of C27H27Cl3N6. It has a CAS number of 69235-50-3. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for Acriflavine hydrochloride is limited. As an antiseptic, it is used topically at low concentrations. As a research compound, Acriflavine hydrochloride is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| 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 hydrochloride (CAS 69235-50-3) is a synthetic acridine compound with antiseptic, antimicrobial, and antiviral activities. It is a potent inhibitor of SARS-CoV-2 PLpro. It has a molecular formula of C27H27Cl3N6 and a molecular weight of 541.90 g/mol. Acriflavine hydrochloride is for research use only. |
| Molecular Formula |
C27H28CL4N6
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|---|---|
| Molecular Weight |
578.363
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| Exact Mass |
576.112
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| CAS # |
69235-50-3
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| Related CAS # |
Acriflavine;8048-52-0
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| PubChem CID |
443101
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| Appearance |
Brown to reddish brown solid powder
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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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| 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, 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)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~46.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.61 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (4.61 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7290 mL | 8.6451 mL | 17.2903 mL | |
| 5 mM | 0.3458 mL | 1.7290 mL | 3.4581 mL | |
| 10 mM | 0.1729 mL | 0.8645 mL | 1.7290 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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