Dyclonine hydrochloride
Based on 1 publication(s) in Google Scholar
Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.12%
- CAS. Nr.: 536-43-6
- Formel: C18H28ClNO2
- Molecular Weight:325.87
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Dyclonine hydrochloride
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Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
TRPV3 |
ALDH2 |
ALDH3A1 |
AChE |
In Vitro
Dyclonine inhibits the proliferation of cultured cardiomyocytes at concentrations of 1-10 μM by suppressing ALDH2; it also inhibits the proliferation of HSC4 oral squamous cell carcinoma cells cultured in vitro, and restores the sensitivity of drug-resistant HSC4 cells to Sulfasalazine (HY-14655) via ALDH inhibition[1].
Dyclonine (0.3-10 μM; 48 h) dose-dependently increases the FXN protein level in lymphoblasts derived from Friedreich's ataxia (FA)[2].
Dyclonine (3-30 μM; 24 h) dose-dependently increases the level of FXN transcripts in lymphoblasts derived from Friedreich's ataxia (FA) patients, reaching a maximum induction of approximately 3.2-fold after treatment with 30 μM for 24 h, and exhibits a stronger inductive effect in cells with longer GAA repeat sequences[2].
Dyclonine (5 μM; 24 h) enhances the binding of Nrf2 to the conserved ARE site in the FXN locus in lymphoblasts from FA patients[2].
Dyclonine (1-10 μM) dose-dependently inhibits the activity of histone methyltransferase G9a in nuclear extracts of healthy lymphoblasts; it also rescues the aconitase activity defect in lymphoblasts derived from Fanconi anemia (FA)[2].
Dyclonine (3-30 μM; with 1 mM 2-APB (HY-W009724)) modulates the inhibitory potency against mouse TRPV3 channels overexpressed in HEK 293T cells, and this regulatory effect relies on amino acid residues located in the channel pore region. Relative to wild-type TRPV3 with an IC50 value of 3.2 μM, L630W, N643A, I644W and L655A mutations reduce its inhibitory capacity, whereas L642A and I659A mutations strengthen its channel-blocking activity[3].
Dyclonine (1.25-10 μM; 24 h) dose-dependently activates the Nrf2/ARE pathway in stable HeLa-ARE-luciferase cells, and luciferase activity is induced to approximately 2.5-fold after treatment with 10 μM for 24 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dyclonine facilitates oligodendrogenesis, remyelination and the conversion of regenerative microglia upon oral delivery in mouse models with drug-triggered brain demyelination lesions[1].
Dyclonine (1-50 μM; intradermal injection; single administration) dose-dependently ameliorates TRPV3-mediated acute pruritus in mice, with the highest tested dose (50 μM) reducing the number of carvacrol (HY-N0711)-induced scratching bouts to 18.0 within 30 min[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 536-43-6
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Appearance Solid
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Molecular Weight 325.87
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Formel C18H28ClNO2
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Color White to off-white
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SMILES
O=C(C1=CC=C(OCCCC)C=C1)CCN2CCCCC2.Cl
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Synonyms
Dyclocaine hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Elife
Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine. [Abstract]2021 Apr 20:10:e68128. PMID: 33876725
Lösungsmittel & Löslichkeit
In Vitro:
H2O : 50 mg/mL (153.44 mM; Need ultrasonic)
DMSO : ≥ 25 mg/mL (76.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (295 KB)
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SDS (585 KB)
- English - EN (585 KB)
- Français - FR (585 KB)
- Deutsch - DE (585 KB)
- Norwegian - NO (585 KB)
- Español - ES (585 KB)
- Swedish - SV (585 KB)
- Italian - IT (585 KB)
- Korean - KR (585 KB)
- Portuguese - PT (585 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Bailly C, et al. A new horizon for the anesthetic drug dyclonine. Biochemical pharmacology. 2026 Feb;244:117569. [Content Brief]
[2]. Sahdeo S, et al. Dyclonine rescues frataxin deficiency in animal models and buccal cells of patients with Friedreich's ataxia. Human molecular genetics. 2014 Dec 20;23(25):6848-62. [Content Brief]
[3]. Liu Q, et al. Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine. eLife. 2021 Apr 20;10:e68128. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.0687 mL | 15.3435 mL | 30.6871 mL | 76.7177 mL |
| 5 mM | 0.6137 mL | 3.0687 mL | 6.1374 mL | 15.3435 mL | |
| 10 mM | 0.3069 mL | 1.5344 mL | 3.0687 mL | 7.6718 mL | |
| 15 mM | 0.2046 mL | 1.0229 mL | 2.0458 mL | 5.1145 mL | |
| 20 mM | 0.1534 mL | 0.7672 mL | 1.5344 mL | 3.8359 mL | |
| 25 mM | 0.1227 mL | 0.6137 mL | 1.2275 mL | 3.0687 mL | |
| 30 mM | 0.1023 mL | 0.5115 mL | 1.0229 mL | 2.5573 mL | |
| 40 mM | 0.0767 mL | 0.3836 mL | 0.7672 mL | 1.9179 mL | |
| 50 mM | 0.0614 mL | 0.3069 mL | 0.6137 mL | 1.5344 mL | |
| 60 mM | 0.0511 mL | 0.2557 mL | 0.5115 mL | 1.2786 mL | |
| H2O | 80 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9590 mL |
| 100 mM | 0.0307 mL | 0.1534 mL | 0.3069 mL | 0.7672 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Dyclonine hydrochloride Related Classifications
HY-B0364A Related Classifications
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