2. Others Metabolic Enzyme/Protease
  3. Drug Derivative Cytochrome P450
  4. Dimethocaine

Dimethocaine  (Synonyms: Larocaine)

製品番号: HY-121870 純度: 99.58%
COA 取扱説明書 Technical Support

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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Dimethocaine

Dimethocaine 構造式

CAS 番号 : 94-15-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
25 mg $25 在庫あり
50 mg $35 在庫あり
100 mg $52 在庫あり
500 mg $105 在庫あり
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Dimethocaine 関連抗体

Top Publications Citing Use of Products

Cytochrome P450 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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製品説明

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[1][2].

IC50 & Target[1]

CYP1A2

 

CYP2C19

 

CYP2D6

 

CYP3A4

 

体外実験

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.

Dimethocaine 関連抗体
体内実験

Dimethocaine (10-40 mg/kg; i.p.; single acute administration) produces significant locomotor stimulation, conditioned place preference-based reinforcing effects, as well as dose-dependent anxiogenic-like effects or altered open-arm exploratory behavior in male Swiss mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Swiss mice (male, ≈30 g)[2]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.p.; single acute dose
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.
分子量

278.39

分子式

C16H26N2O2
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(COC(C1=CC=C(C=C1)N)=O)CN(CC)CC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5921 mL 17.9604 mL 35.9208 mL
5 mM 0.7184 mL 3.5921 mL 7.1842 mL
10 mM 0.3592 mL 1.7960 mL 3.5921 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.90%

COA (243 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

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
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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Dimethocaine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dimethocaine94-15-5LarocaineDrug DerivativeCytochrome P450Drug derivativeCYPsmale Swiss miceP450 1A2N-acetylationdopamine transporterP450 3A4P450 2C19NAT2dopaminergic activityhuman liver microsomesP450 2D6Inhibitorinhibitorinhibit

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