Aripiprazole lauroxil 是一种长效注射剂 (LAI) 的抗精神病药物,是阿立哌唑的 N-酰氧基甲基前药形式。它能够被体内酯酶裂解为 N-羟甲基阿立哌唑(月桂酸),再裂解为阿立哌唑,无毒性。
产品描述
Aripiprazole lauroxil, the N-acyloxymethyl prodrug form of aripiprazole, a long-acting injectable (LAI) antipsychotic. Aripiprazole lauroxil is cleaved by esterases in vivo to N-hydroxymethyl aripiprazole (lauric acid), which is then cleaved to aripiprazole, which is non-toxic.
体内活性
Intravenous administration of 1.87?mg/ml Aripiprazole lauroxil 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].
Cas No.
1259305-29-7
分子式
C36H51Cl2N3O4
分子量
660.71
别名
Aripiprazole Lauroxil
储存和溶解度
DMSO:8 mg/mL (12.11 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years