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5g |
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10g |
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Other Sizes |
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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].
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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].
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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. |
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. |
References |
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Additional Infomation |
Dyclonine Hydrochloride is the hydrochloride salt of Dyclonine, an unclassified compound with local anesthetic effect. Dyclonine reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation. This reversibly stabilizes the membrane and inhibits depolarization, leading to the failure of a propagated action potential and subsequent conduction blockade. This results in a transient and reversible loss of sensation in a localized area of the body.
See also: Dyclonine (has active moiety); Benzethonium Chloride; Dyclonine Hydrochloride (component of); Dyclonine hydrochloride; menthol; pectin (component of) ... View More ... |
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.