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Purity: ≥98%
Aripiprazole lauroxil (RDC3317; RDC-3317; ALKS 9070; ALKS-9072; Abilify; Aristada) is a long-acting injectable atypical antipsychotic approved in 2015 by FDA mainly for the treatment of schizophrenia and bipolar disorder. It can also be used as an add-on treatment in major depressive disorder, tic disorders and irritability associated with autism. Aripiprazole lauroxil is an N-acyloxymethyl prodrug of aripiprazole that is administered via intramuscular injection once every four to six weeks for the treatment of schizophrenia.
| ln Vivo |
The intermediate N-corresponding aripiprazole is involved in the in vivo biotransformation of aripiprazole lauroxil (in-vehicle product; 1.87 mg/mL). Thus, Aripiprazole lauroxil has a high rate of biotransformation, resulting in the synthesis of the observed N-corresponding methyl aripiprazole, according to peripheral data. When animals are given Aristrozole Lauroyl, the concentrations of Aristrozole are very high [1].
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| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rats[1]
Doses: 1.87 mg/ml Route of Administration: Blood samples were collected at 5, 15, 30 minutes and 1, 2, 4, 6, 8 and 24 hrs (hrs (hours)) after administration. Experimental Results: Displayed clearance: 0.32 ± 0.11 L/h/kg. |
| References |
[1]. Jann MW, et al. Long-Acting Injectable Second-Generation Antipsychotics: An Update and Comparison Between Agents.CNS Drugs. 2018 Mar;32(3):241-257.
[2]. Rohde M, et al. Biological conversion of aripiprazole lauroxil - An N-acyloxymethyl aripiprazole prodrug.Results Pharma Sci. 2014 May 2;4:19-25. |
| Molecular Formula |
C36H51N3O4CL2
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|---|---|
| Molecular Weight |
660.714
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| CAS # |
1259305-29-7
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| Related CAS # |
129722-12-9;851220-85-4 (hydrate);1259305-26-4 (cavoxil);1259305-29-7 (lauroxil);
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| SMILES |
CCCCCCCCCCCC(=O)OCN1C2=C(C=CC(=C2)OCCCCN3CCN(CC3)C4=CC=CC(=C4Cl)Cl)CCC1=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~8.33 mg/mL (~12.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1514 mL | 0.7568 mL | 1.5135 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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