Dimethocaine
Based on 1 Customer Validation
Dimethocaine (Larocaine) is a cocaine derivative and ester-type local anesthetic. Dimethocaine is metabolized by hP450 1A2, 2C19, 2D6, and 3A4 in vitro. Dimethocaine exhibits locomotor-promoting, reinforcing, and anxiogenic effects.
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- Pureté: 99.58%
- CAS No.: 94-15-5
- Formule: C16H26N2O2
- Masse moléculaire:278.39
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CYP1A2 |
CYP2C19 |
CYP2D6 |
CYP3A4 |
Dimethocaine (25 μM; 30 min) is metabolized in vitro by baculovirus-expressed hP450 1A2, 2C19, 2D6 and 3A4, while no significant activity is observed with other tested P450 subtypes[1].
Dimethocaine (50 μM; 20 min) undergoes N-acetylation modification by baculovirus-expressed hNAT2 in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (male, ≈30 g)[2]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.p.; single acute dose
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Result:Produced a significant, dose-dependent increase in locomotor activity counts compared to controls (one-way ANOVA: F(3,43)=6.92, P<0.001).
Induced stereotypic movements mainly at the 40 mg/kg dose.
Induced a significant preference for the drug-paired compartment compared to controls (one-way ANOVA: F(3,41)=9.74, P<0.0002).
Showed a negative relationship between dose and time spent in the drug-paired compartment.
Reduced the relative number of open arm entries and percent time spent on open arms at 10 and 20 mg/kg doses compared to controls (one-way ANOVA for percent open arm time: F(3,34)=17.3, P<0.0001).
Increased the relative number of open arm entries and percent time spent on open arms at the 40 mg/kg dose compared to controls.
Chemical Information
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CAS No. 94-15-5
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Appearance Solid
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Masse moléculaire 278.39
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Formule C16H26N2O2
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Color Light yellow to yellow
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SMILES
CC(C)(COC(C1=CC=C(C=C1)N)=O)CN(CC)CC
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Synonyms
Larocaine
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 130 mg/mL (466.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.17 mg/mL (7.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (7.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Meyer MR, et al. Dimethocaine, a synthetic cocaine derivative: studies on its in vitro metabolism catalyzed by P450s and NAT2. Toxicol Lett. 2014;225(1):139-146. [Content Brief]
[2]. Rigon AR, et al. Stimulant activities of dimethocaine in mice: reinforcing and anxiogenic effects. Psychopharmacology (Berl). 1996;127(4):323-327. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.5921 mL | 17.9604 mL | 35.9208 mL | 89.8021 mL |
| 5 mM | 0.7184 mL | 3.5921 mL | 7.1842 mL | 17.9604 mL | |
| 10 mM | 0.3592 mL | 1.7960 mL | 3.5921 mL | 8.9802 mL | |
| 15 mM | 0.2395 mL | 1.1974 mL | 2.3947 mL | 5.9868 mL | |
| 20 mM | 0.1796 mL | 0.8980 mL | 1.7960 mL | 4.4901 mL | |
| 25 mM | 0.1437 mL | 0.7184 mL | 1.4368 mL | 3.5921 mL | |
| 30 mM | 0.1197 mL | 0.5987 mL | 1.1974 mL | 2.9934 mL | |
| 40 mM | 0.0898 mL | 0.4490 mL | 0.8980 mL | 2.2451 mL | |
| 50 mM | 0.0718 mL | 0.3592 mL | 0.7184 mL | 1.7960 mL | |
| 60 mM | 0.0599 mL | 0.2993 mL | 0.5987 mL | 1.4967 mL | |
| 80 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1225 mL | |
| 100 mM | 0.0359 mL | 0.1796 mL | 0.3592 mL | 0.8980 mL |
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