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Dehydroaripiprazole

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Catalog No. T10989Cas No. 129722-25-4
Alias OPC-14857, DM-14857

Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has antipsychotic activity equivalent to aripiprazole.

Dehydroaripiprazole

Dehydroaripiprazole

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Purity: 98.7%
Catalog No. T10989Alias OPC-14857, DM-14857Cas No. 129722-25-4
Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has antipsychotic activity equivalent to aripiprazole.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31-In Stock
5 mg$72-In Stock
10 mg$122-In Stock
25 mg$247-In Stock
50 mg$368-In Stock
100 mg$543-In Stock
500 mg$1,160-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.7%
Appearance:Solid
Color:Yellow
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Product Introduction

Dehydroaripiprazole AI Summary
Dehydroaripiprazole exhibits post-synaptic dopamine autoreceptor antagonist activity, inhibiting apomorphine-induced stereotyped behavior in mice with an ED50 of 0.9 umol.kg-1, and shows inhibition of GBL-induced DOPA accumulation, indicating dopamine autoreceptor agonist activity with an ED50 greater than 22.0 umol.kg-1. Furthermore, it demonstrates alpha-1 adrenoceptor antagonist activity by inhibiting the lethal effects of noradrenaline in mice, with an ED50 greater than 287.0 umol.kg-1. In human cellular assays, Dehydroaripiprazole functions as a potent agonist at the D2L receptor, demonstrating beta-arrestin recruitment and inhibition of isoproterenol-stimulated cAMP production, with EC50 values of 6.3 nM and 158.0 nM, respectively. It also shows a high affinity for the D2L receptor by displacing [3H]N-methylspiperone with a Ki value of 7.3 nM. These bioactivities indicate that Dehydroaripiprazole has significant therapeutic potential..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has antipsychotic activity equivalent to aripiprazole.
Targets&IC50
5-HT1A:4.2 nM (ki)
SynonymsOPC-14857, DM-14857
Chemical Properties
Molecular Weight446.37
FormulaC23H25Cl2N3O2
Cas No.129722-25-4
SmilesClc1cccc(N2CCN(CCCCOc3ccc4=CCC(=O)N=c4c3)CC2)c1Cl
Relative Density.1.281 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 11 mg/mL (24.64 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.24 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2403 mL11.2015 mL22.4029 mL112.0147 mL
5 mM0.4481 mL2.2403 mL4.4806 mL22.4029 mL
10 mM0.2240 mL1.1201 mL2.2403 mL11.2015 mL
20 mM0.1120 mL0.5601 mL1.1201 mL5.6007 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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