Aripiprazolelauroxil，阿立哌唑的N-酰氧基甲基前药形式，一种长效注射剂(LAI)的抗精神病药物。Aripiprazolelauroxil被体内酯酶裂解为N-羟甲基阿立哌唑(月桂酸)，再裂解为阿立哌唑，无毒。
货号:ajcx30190
CAS:1259305-29-7
分子式:C36H51Cl2N3O4
分子量：660.71
溶解度:DMSO: 8.33 mg/mL (12.61 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.