yingweiwo

Dyclonine Hydrochloride

Alias: Dyclone; Dyclonine HCL; Dyclonine Hydrochloride
Cat No.:V20317 Purity: ≥98%
Dyclonine (Dyclocaine) HCl is an orally bioavailable covalent/irreversible inhibitor of ALDH (can cross the BBB (blood-brain barrier)) with IC50s of 35 and 76 µM for ALDH2 and ALDH3A1 respectively.
Dyclonine Hydrochloride
Dyclonine Hydrochloride Chemical Structure CAS No.: 536-43-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5g
10g
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Product Description
Dyclonine (Dyclocaine) HCl is an orally bioavailable covalent/irreversible inhibitor of ALDH (can cross the BBB (blood-brain barrier)) with IC50s of 35 and 76 µM for ALDH2 and ALDH3A1 respectively. Dyclonine HCl has sensitizing activity targeting cancer/tumor cells and antimicrobial effect. Dyclonine HCl is also a local anesthetic that blocks the conduction of a variety of nerve impulses or stimuli and inhibits touch and pain sensations.
Biological Activity I Assay Protocols (From Reference)
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].
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].
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

[1]. Synthetic lethality of the ALDH3A1 inhibitor dyclonine and xCT inhibitors in glutathione deficiency-resistant cancer cells. Oncotarget. 2018 Sep 18;9(73):33832-33843.

[2]. Antimicrobial properties of dyclonine hydrochloride, a new topical anesthetic. J Am Pharm Assoc Am Pharm Assoc. 1956 May;45(5):320-5.

[3]. Discovery of a novel class of covalent inhibitor for aldehyde dehydrogenases. J Biol Chem. 2011 Dec 16;286(50):43486-94.

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 ...
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H28CLNO2
Molecular Weight
325.87
Exact Mass
325.18
CAS #
536-43-6
Related CAS #
Dyclonine-d9 hydrochloride
PubChem CID
68304
Appearance
White to off-white solid powder
Boiling Point
424.5ºC at 760 mmHg
Melting Point
175-176°C
Flash Point
210.5ºC
LogP
4.664
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
8
Heavy Atom Count
22
Complexity
292
Defined Atom Stereocenter Count
0
InChi Key
KNZADIMHVBBPOA-UHFFFAOYSA-N
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
Chemical Name
1-(4-butoxyphenyl)-3-piperidin-1-ylpropan-1-one;hydrochloride
Synonyms
Dyclone; Dyclonine HCL; Dyclonine Hydrochloride
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
H2O : ~50 mg/mL (~153.44 mM)
DMSO : ≥ 25 mg/mL (~76.72 mM)
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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

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.

Contact Us