Aripiprazole Lauroxil |
カタログ番号GC60598
One-Click Copy Product Info
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アリピプラゾールの N-アシルオキシメチル プロドラッグであるアリピプラゾール ラウロキシルは、統合失調症に対する長時間作用型注射剤（LAI）の定型抗精神病薬です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1259305-29-7
Sample solution is provided at 25 µL, 10mM.
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Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body's enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity[1].
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]. Animal Model: Female Sprague Dawley rats[1]
[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.
| Cas No. | 1259305-29-7 | SDF | |
| Canonical SMILES | CCCCCCCCCCCC(OCN1C(CCC2=C1C=C(OCCCCN3CCN(C4=CC=CC(Cl)=C4Cl)CC3)C=C2)=O)=O | ||
| Formula | C36H51Cl2N3O4 | M.Wt | 660.71 |
| 溶解度 | DMSO: 8.33 mg/mL (12.61 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5135 mL | 7.5676 mL | 15.1352 mL |
| 5 mM | 302.7 μL | 1.5135 mL | 3.027 mL |
| 10 mM | 151.4 μL | 756.8 μL | 1.5135 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)