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| 5g |
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| 10g |
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| Other Sizes |
| Targets |
Dyclonine Hydrochloride targets multiple proteins and pathways. As a local anesthetic, it blocks voltage-gated sodium channels on nerve cell membranes, inhibiting the transmission of pain signals. As a covalent/irreversible inhibitor, it targets aldehyde dehydrogenases (ALDH), specifically ALDH2 and ALDH3A1. ALDH enzymes are involved in the detoxification of aldehydes and are overexpressed in certain cancer stem cells, contributing to drug resistance.
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| ln Vitro |
Cancer cells are made more susceptible to glutathione and cysteine deficiencies by dyclonine hydrochloride (50 µM; 24 hours) [1]. Significant bactericidal and fungicidal efficacy is demonstrated by dyclonine hydrochloride (0–2048 µg/mL; 24 or 48 hours) [2].
In vitro, dyclonine hydrochloride (50 µM; 24 hours) sensitizes cancer cells to glutathione and cysteine deficiencies. It demonstrates significant bactericidal and fungicidal efficacy (0-2048 µg/mL; 24 or 48 hours). The minimum bactericidal concentrations against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Trichophyton mentagrophytes are 0.006%, 0.025%, 0.012%, and 0.025%, respectively. |
| ln Vivo |
Treatment with in vivo sulfasalazine sensitizes involucrin+ differentiated tumor cells to dyclonine hydrochloride (5 mg/kg; i.p.; once daily for 24 days) [1]. Tumor growth caused by ALDH3A1-expressing gastric cancer stem-like cells is inhibited by a combination of sulfasalazine and dyclonine hydrochloride (5 mg/kg; intraperitoneal injection; once daily for 21 days) [1].
In vivo, dyclonine hydrochloride (5 mg/kg; intraperitoneal; once daily) has been studied in combination with sulfasalazine in mouse models. It inhibits tumor growth caused by ALDH3A1-expressing gastric cancer stem-like cells when combined with sulfasalazine. It also enhances the anti-tumor effects of sulfasalazine on HNSCC tumors. These findings suggest a potential role in cancer therapy. |
| Enzyme Assay |
In vitro enzyme assays for dyclonine hydrochloride measure its inhibition of ALDH2 and ALDH3A1 activities. Recombinant ALDH enzymes are incubated with a substrate (e.g., propionaldehyde) and NAD⁺. The production of NADH is measured spectrophotometrically at 340 nm. Various concentrations of dyclonine are added to determine IC50 values. Selectivity for ALDH isoforms can be assessed.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HSC-4 Cell Tested Concentrations: 50 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited ALDH activity and induced 4-HNE accumulation in GSH-depleted cancer cells. Cell viability assay[2] Cell Types: Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Trichomonas mentagrophytes Tested Concentrations: 0-2048 µg/mL Incubation Duration: 24 hrs (hours) (bacteria), 48 hrs (hours) (fungi) Experimental Results: demonstrated Good antibacterial and antifungal activity, the minimum bactericidal concentrations against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Trichoderma mentaphysalis are 0.006%, 0.025%, 0.012%, and 0.025% respectively. Cellular assays for dyclonine hydrochloride use cancer cell lines, such as HSC-4 cells. Cells are treated with 50 µM dyclonine for 24 hours. ALDH activity is assessed using an ALDH activity assay kit or by flow cytometry with an ALDH substrate (ALDEFLUOR). Cell viability is measured using MTT or ATP-lite assays. The accumulation of 4-HNE (a marker of oxidative stress) can be measured. |
| Animal Protocol |
Animal/Disease Models: Athymic nude mice (HSC-2 cell implantation model) [1].
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 24 days (combined with sulfasalazine). Experimental Results: Combination with sulfasalazine attenuated tumor formation of HSC-2 cells transplanted into nude mice. Animal/Disease Models: C57BL6 mouse (K19-Wnt1/C2mE-KP cell implantation model) [1]. Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 21 days (combined with sulfasalazine). Experimental Results: Enhanced anti-tumor effects of sulfasalazine on HNSCC tumors composed of CD44v high stem-like tumor cells and epithelial+ differentiated tumor cells. In vivo animal studies for dyclonine hydrochloride are conducted in athymic nude mice or C57BL6 mice bearing tumor xenografts. Dyclonine (5 mg/kg) is administered intraperitoneally once daily, in combination with sulfasalazine. Tumor volume is measured over time. Tumor formation and growth are assessed. Efficacy is compared to vehicle and monotherapy groups. |
| ADME/Pharmacokinetics |
Dyclonine Hydrochloride has a molecular weight of 325.87 g/mol and a molecular formula of C18H27NO2·HCl. It is a white crystalline powder. It is typically stored at room temperature. It is soluble in water and alcohol. It is orally bioavailable and can cross the blood-brain barrier (BBB).
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| Toxicity/Toxicokinetics |
Dyclonine Hydrochloride is generally well-tolerated when used topically as a local anesthetic. Systemic toxicity is rare. However, as an ALDH inhibitor, it may have off-target effects. In combination with sulfasalazine, it shows anti-tumor activity in preclinical models. Comprehensive toxicity data is available from its use as a local anesthetic. It is an approved over-the-counter drug for topical use.
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| References |
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| Additional Infomation |
Dyclonine hydrochloride is the hydrochloride salt of Dyclonine, an unclassified local anesthetic compound. Dyclonine reversibly binds to activated sodium channels on neuronal membranes, thereby reducing the permeability of the neuronal membrane to sodium ions, leading to an increase in the excitation threshold. This reversibly stabilizes the cell membrane and inhibits depolarization, preventing action potential propagation and thus blocking conduction. This results in a transient and reversible loss of sensation in a localized area of the body.
See also: Dyclonine (contains active ingredient); Benzalkonium chloride; Dyclonine hydrochloride (ingredient); Dyclonine hydrochloride; Menthol; Pectin (ingredient)...See more... Dyclonine Hydrochloride is a local anesthetic and an ALDH inhibitor. It has IC50s of 35 µM and 76 µM for ALDH2 and ALDH3A1, respectively. It has antimicrobial effects and sensitizes cancer cells. It is used as an over-the-counter throat lozenge for local anesthesia. |
| Molecular Formula |
C18H28CLNO2
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| Molecular Weight |
325.87
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| Exact Mass |
325.18
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| CAS # |
536-43-6
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| Related CAS # |
Dyclonine-d9 hydrochloride
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| PubChem CID |
68304
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| Appearance |
White to off-white solid powder
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| Boiling Point |
424.5ºC at 760 mmHg
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| Melting Point |
175-176°C
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| Flash Point |
210.5ºC
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| LogP |
4.664
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
292
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KNZADIMHVBBPOA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H27NO2.ClH/c1-2-3-15-21-17-9-7-16(8-10-17)18(20)11-14-19-12-5-4-6-13-19;/h7-10H,2-6,11-15H2,1H3;1H
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| Chemical Name |
1-(4-butoxyphenyl)-3-piperidin-1-ylpropan-1-one;hydrochloride
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| Synonyms |
Dyclone; Dyclonine HCL; Dyclonine Hydrochloride
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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) |
H2O : ~50 mg/mL (~153.44 mM)
DMSO : ≥ 25 mg/mL (~76.72 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.67 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 (7.67 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 (7.67 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 | 3.0687 mL | 15.3435 mL | 30.6871 mL | |
| 5 mM | 0.6137 mL | 3.0687 mL | 6.1374 mL | |
| 10 mM | 0.3069 mL | 1.5344 mL | 3.0687 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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