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Product Data Sheet Product data sheet MedKoo Cat#: 326728 Name: Aripiprazole lauroxil CAS#: 1259305-29-7 (lauroxil) Chemical Formula: C36H51Cl2N3O4 Exact Mass: 659.3257 Molecular Weight: 660.721 Product supplied as: Powder Purity (by HPLC): ≥ 98% Shipping conditions Ambient temperature Storage conditions: Powder: -20°C 3 years; 4°C 2 years. In solvent: -80°C 3 months; -20°C 2 weeks. 1. Product description: Aripiprazole lauroxil, aslo known as RDC 3317, is a long-acting injectable atypical antipsychotic. It is an N-acyloxymethyl prodrug of aripiprazole that is administered via intramuscular injection once every four to six weeks for the treatment of schizophrenia. Aripiprazole lauroxil was approved by the U.S. FDA on 5 October 2015. 2. CoA, QC data, SDS, and handling instruction SDS and handling instruction, CoA with copies of QC data (NMR, HPLC and MS analytical spectra) can be downloaded from the product web page under “QC And Documents” section. Note: copies of analytical spectra may not be available if the product is being supplied by MedKoo partners. Whether the product was made by MedKoo or provided by its partners, the quality is 100% guaranteed. 3. Solubility data Solvent Max Conc. mg/mL Max Conc. mM DMSO 8.33 12.61 4. Stock solution preparation table: Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg 1 mM 1.51 mL 7.57 mL 15.13 mL 5 mM 0.30 mL 1.51 mL 3.03 mL 10 mM 0.15 mL 0.76 mL 1.51 mL 50 mM 0.03 mL 0.15 mL 0.30 mL 5. Molarity Calculator, Reconstitution Calculator, Dilution Calculator Please refer the product web page under section of “Calculator” 6. Recommended literature which reported protocols for in vitro and in vivo study In vitro study 1. Badran A, Tul-Wahab A, Zafar H, Mohammad N, Imad R, Ashfaq Khan M, Baydoun E, Choudhary MI. Antipsychotics drug aripiprazole as a lead against breast cancer cell line (MCF-7) in vitro. PLoS One. 2020 Aug 3;15(8):e0235676. doi: 10.1371/journal.pone.0235676. PMID: 32746451; PMCID: PMC7398703. 2. Kim MS, Yoo BC, Yang WS, Han SY, Jeong D, Song JM, Kim KH, Aravinthan A, Kim JH, Kim JH, Kim SC, Cho JY. Src is the primary target of aripiprazole, an atypical antipsychotic drug, in its anti-tumor action. Oncotarget. 2017 Dec 8;9(5):5979-5992. doi: 10.18632/oncotarget.23192. PMID: 29464048; PMCID: PMC5814188. In vivo study 1. Rizzo F, Nespoli E, Abaei A, Bar-Gad I, Deelchand DK, Fegert J, Rasche V, Hengerer B, Boeckers TM. Aripiprazole Selectively Reduces Motor Tics in a Young Animal Model for Tourette's Syndrome and Comorbid Attention Deficit and Hyperactivity Disorder. Front Neurol. 2018 Feb 13;9:59. doi: 10.3389/fneur.2018.00059. PMID: 29487562; PMCID: PMC5816975. 2. Pan B, Chen J, Lian J, Huang XF, Deng C. Unique Effects of Acute Aripiprazole Treatment on the Dopamine D2 Receptor Downstream cAMP-PKA and Akt-GSK3β Signalling Pathways in Rats. PLoS One. 2015 Jul 10;10(7):e0132722. doi: 10.1371/journal.pone.0132722. PMID: 26162083; PMCID: PMC4498891. MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831 Product data sheet 7. Bioactivity Biological target: Aripiprazole lauroxil is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. In vitro activity In conclusion, aripiprazole inhibits cell proliferation in breast cancer MCF-7 cells line in a concentration dependent manner. Mechanistic studies indicated that the anti-cancer effect of aripiprazole may be due to an enhanced apoptosis in MCF-7 cells line. This was further supported by observing increased nuclear condensation in MCF-7 cells line. The drug inhibited cell cycle progression in subG0G1 phase. Aripiprazole also increased the expression of certain pro-apoptotic genes (caspases 3, and BCL10), while expression of anti-apoptotic genes (BCL2L1, and c-myc) that are involved in the progression of breast cancer were decreased. This study thus indicated that aripiprazole inhibit the cancer cell proliferation through apoptosis. Further studies, however, are required to study the effect of aripiprazole on intrinsic or extrinsic pathways of apoptosis, as well as to enhance its activity by structural modifications. Reference: PLoS One. 2020; 15(8): e0235676. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7398703/ In vivo activity The present study demonstrated the in vivo effects of aripiprazole on the downstream pathways of the D2R, by comparing it with haloperidol and bifeprunox. The results of the current study showed that aripiprazole had similar effects on PKA subunits to haloperidol, but not bifeprunox in the CPu and VTA, indicating that relatively lower intrinsic activity of aripiprazole on D2R might be the mechanism of aripiprazole to exert its therapeutic effects on treating positive symptoms of schizophrenia; on the other hand, aripiprazole displayed a very different action mode on the GSK3β activity from the other two chemicals, probably explaining its therapeutic effects on both positive and negative symptoms of schizophrenia, with reduced EPS. Together, these in vivo findings suggest that the relatively low intrinsic activity at D2R might be the reason that aripiprazole possesses unique pharmacological profiles and clinical effects from the other antipsychotic drugs. Reference: PLoS One. 2015; 10(7): e0132722. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4498891/ Note: The information listed here was extracted from literature. MedKoo has not independently retested and confirmed the accuracy of these methods. Customer should use it just for a reference only. MedKoo Biosciences || http://www.medkoo.com || [email protected] 2500 Gateway Centre Blvd Suite 400, Morrisville, NC27560, USA. Tel: 919-636-5577, Fax: 919-980-4831 .
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