2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Aripiprazole Lauroxil

Aripiprazole lauroxil, an N-acyloxymethyl proagent of Aripiprazole (HY-14546), is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia and a ligand of dopamine receptor D2R/D4R. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.

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Aripiprazole Lauroxil

Aripiprazole Lauroxil Chemical Structure

CAS No. : 1259305-29-7

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Based on 2 publication(s) in Google Scholar

Other Forms of Aripiprazole Lauroxil:

Aripiprazole Lauroxil Related Antibodies

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2 Publications Citing Use of MCE Aripiprazole Lauroxil

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Description

Aripiprazole lauroxil, an N-acyloxymethyl proagent of Aripiprazole (HY-14546), is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia and a ligand of dopamine receptor D2R/D4R. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.

In Vivo

Aripiprazole lauroxil (intravenous administration; 1.87 mg/ml) bioconversion in vivo involves the formation of an intermediate, N-hydroxymethyl aripiprazole, the in vitro data indicates a high bioconversion of aripiprazole lauroxil, thus, the concentration of N-hydroxymethyl aripiprazole observed in the animals dosed with aripiprazole lauroxil is surprisingly high[1].

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

Animal Model: Female Sprague Dawley rats[1]
Dosage: 1.87 mg/ml 
Administration: Blood samples is taken at 5, 15, 30 min and 1, 2, 4, 6, 8 and 24 h after administration
Result: Exhibits an clearance: 0.32 ± 0.11 L/h/kg. 
Essai clinique
Masse moléculaire

660.71

Formule

C36H51Cl2N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCCCCCC(OCN1C(CCC2=C1C=C(OCCCCN3CCN(C4=CC=CC(Cl)=C4Cl)CC3)C=C2)=O)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 8.33 mg/mL (12.61 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 1.5135 mL 7.5676 mL 15.1352 mL
5 mM 0.3027 mL 1.5135 mL 3.0270 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.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.83 mg/mL (1.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Pureté et documentation
Références

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 1.5135 mL 7.5676 mL 15.1352 mL 37.8381 mL
5 mM 0.3027 mL 1.5135 mL 3.0270 mL 7.5676 mL
10 mM 0.1514 mL 0.7568 mL 1.5135 mL 3.7838 mL
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Aripiprazole Lauroxil Related Classifications

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:

Aripiprazole Lauroxil1259305-29-7Dopamine ReceptorAristada schizophreniaInhibitorinhibitorinhibit

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