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| Other Sizes |
| Targets |
Induces lysosomal damage, leading to the release of lysosomal enzymes including phospholipases, which in turn initiate prostaglandin synthesis. [1]
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| ln Vitro |
Acridine has a MIC range of 100-200 μg/mL and is effective against Staphylococcus aureus, including MRSA. The MIC of Acridine against E. Proteus vulgaris and Proteus mirabilis have MICs more than 1,600 μg/mL, whereas coli is 200–800 μg/mL[3].
Acrinol showed strong antibacterial activity against Gram-positive cocci. It inhibited all tested strains of Staphylococcus aureus (including MRSA) at 200 μg/mL, and all tested Gram-positive strains at 400 μg/mL. [3] Against Gram-negative rods, Acrinol was less effective. It inhibited 77.1% (37/48) of tested Gram-negative strains (including Escherichia coli, Enterobacter cloacae) at 800 μg/mL. [3] Acrinol inhibited all tested Pseudomonas aeruginosa strains (including multidrug-resistant ones) at 1,600 μg/mL, with MICs ranging from 200 to 1,600 μg/mL. [3] Acrinol did not inhibit Proteus vulgaris, Proteus mirabilis and Morganella morganii even at 1,600 μg/mL. [3] Acrinol exhibited synergistic antibacterial effect with tetracycline against Pseudomonas aeruginosa #40-1. The combination of Acrinol (100 μg/mL) and tetracycline (12.5 μg/mL) inhibited bacterial growth, whereas Acrinol alone required 400 μg/mL and tetracycline alone required 50 μg/mL. The FIC Index was 0.5, indicating synergy. [3] Exposure of Acrinol to light (500 lx for up to 90 days) did not change its MIC against Staphylococcus aureus ATCC 25923 (100 μg/mL) and Escherichia coli ATCC 25922 (200 μg/mL). [3] Light-exposed Acrinol (500 lx, 90 days) still showed synergistic effect with tetracycline against Pseudomonas aeruginosa #40-1 (FIC Index = 0.5), identical to unexposed control. [3] |
| ln Vivo |
Pregnancy can be ended with ethacridine lactate [1].
In five second-trimester pregnant patients with intrauterine fetal death, extraamniotic instillation of Ethacridine lactate (150 mL of 0.1% solution) followed 4 hours later by a single intramuscular injection of sulprostone (500 μg) resulted in successful termination of all pregnancies. The induction-delivery intervals ranged from 8 hours 30 minutes to 14 hours (mean 10 hours 20 minutes). Expulsion was complete in all cases; no patient required curettage, and no cervical lacerations occurred. Continuous intrauterine pressure monitoring in two patients showed minimal rhythmic uterine activity after ethacridine lactate instillation; after sulprostone injection, a prompt and marked rise in baseline tone occurred, lasting 20 minutes, followed by regular rhythmic uterine contractions leading to expulsion of a 1050 g macerated stillbirth and placenta in an intact amniotic sac at 7 hours 50 minutes. [1] |
| Cell Assay |
The minimum inhibitory concentration (MIC) of Acrinol was determined by the agar dilution method. Two-fold serial dilutions of Acrinol were prepared in sterile purified water, and 2 mL of each dilution was mixed with 18 mL of Mueller-Hinton agar medium to prepare agar plates containing specified concentrations. Test bacterial strains were cultured in Mueller-Hinton broth at 37°C for 18 hours to obtain a bacterial suspension of 10⁶ CFU/mL. Ten microliters of this suspension (10⁶ CFU/plate) was spread onto the agar plates containing Acrinol. After incubation at 37°C for 18 hours, the lowest concentration that completely inhibited visible bacterial growth was recorded as the MIC. [3]
The combined effect of Acrinol and tetracycline was examined using the checkerboard method. Mueller-Hinton agar plates containing serial dilutions of Acrinol alone, tetracycline alone, or combinations of both agents at specified concentrations were prepared. A bacterial suspension (10⁶ CFU/mL) of Pseudomonas aeruginosa #40-1 was inoculated (10 μL/plate) and incubated at 37°C for 18 hours. The MIC of each agent alone and in combination was determined. The FIC Index was calculated as (MIC of Acrinol in combination / MIC of Acrinol alone) + (MIC of tetracycline in combination / MIC of tetracycline alone). Synergy was defined as FIC Index ≤ 0.5. [3] |
| Toxicity/Toxicokinetics |
Side effects were minimal: two patients experienced one episode of vomiting each, and one patient had one episode of diarrhea. [1]
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| References |
[1]. Gupta S, et al. Ethacridine lactate -- a safe and effective drug for termination of pregnancy. Indian J Matern Child Health. 1993;4(2):59-61.
[2]. Rotin LE, et al. Erlotinib synergizes with the poly(ADP-ribose) glycohydrolase inhibitor ethacridine in acute myeloid leukemia cells. Haematologica. 2016 Nov;101(11):e449-e453. [3]. Usuki R, et, al. Antibacterial Activity of Acrinol against Organisms Isolated from Clinical Materials and Influence of Light on Antibacterial Activity of Acrinol. Japanese Journal of Pharmaceutical Health Care and Sciences. 2004 Jan; 30(2):72-77. |
| Additional Infomation |
Allyl alcohol is an organic molecular entity and a topical anti-infective agent.
Ethacridine lactate is used in a combination technique for terminating second-trimester pregnancies complicated by intrauterine fetal death. The mechanism is not fully understood but may be mediated by the release of endogenous prostaglandins through lysosomal damage and subsequent phospholipase release. The method combining extraamniotic ethacridine lactate with intramuscular prostaglandin (sulprostone) is described as simple, safe, effective, and inexpensive, with few side effects. The study utilized intrauterine pressure monitoring to document efficacy. [1] |
| Molecular Formula |
C18H21N3O4
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|---|---|
| Molecular Weight |
343.38
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| Exact Mass |
343.153
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| CAS # |
1837-57-6
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| Related CAS # |
Ethacridine lactate monohydrate;6402-23-9
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| PubChem CID |
15789
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
270 °C(lit.)
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| Melting Point |
62-67 °C(lit.)
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| Flash Point |
143 °C
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| Vapour Pressure |
4.72E-11mmHg at 25°C
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| LogP |
3.565
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(O)C(O)=O.NC1=CC2=NC3=CC=C(OCC)C=C3C(N)=C2C=C1
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| InChi Key |
IYLLULUTZPKQBW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15N3O.C3H6O3/c1-2-19-10-4-6-13-12(8-10)15(17)11-5-3-9(16)7-14(11)18-131-2(4)3(5)6/h3-8H,2,16H2,1H3,(H2,17,18)2,4H,1H3,(H,5,6)
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| Chemical Name |
Propanoic acid, 2-hydroxy-, compd. with 7-ethoxy-3,9-acridinediamine (1
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| Synonyms |
NSC-36333 NSC36333NSC 36333
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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 : ~50 mg/mL (~145.61 mM)
H2O : ~12.5 mg/mL (~36.40 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.28 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 (7.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9122 mL | 14.5611 mL | 29.1223 mL | |
| 5 mM | 0.5824 mL | 2.9122 mL | 5.8245 mL | |
| 10 mM | 0.2912 mL | 1.4561 mL | 2.9122 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06487117 | NOT YET RECRUITING | Drug: Huafu Shengji Ointment Drug: ethacridine lactate solution |
Diabetic Foot | Beijing Daxing District Hospital of Integrated Chinese and Western Medicine | 2024-09 | Early Phase 1 |
| NCT03574935 | UNKNOWN STATUS | Drug: External Chinese medicine Drug: External Western medicine |
Diabetic Foot Ulcer, Skin |
Shanghai Yueyang Integrated Medicine Hospital | 2018-07-01 | Phase 2 |
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