Acitretin 是一种维甲酸,可用于银屑病和阿尔兹海默症的研究。
产品描述
Acitretin is a second-generation, systemic retinoid that has been used in the treatment of psoriasis.
体外活性
Acitretin stimulates ADAM10 promoter activity with an EC(50) of 1.5 mM and leads to an increase of mature ADAM10 protein that results in a two- to three-fold increase of the ratio between alpha- and beta-secretase activity in neuroblastoma cells. [1] Acitretin (5-20 μM) impairs mitochondrial phosphorylation efficiency as demonstrated by the decrease in the state 3 respiration and ATP levels, and by the increase in the lag phase of ADP phosphorylation cycle, without affecting the membrane potential. Acitretin induces Ca(2+)-mediated mitochondrial permeability transition (MPT) and decreased the adenine nucleotide translocase (ANT) content. [2] Acitretin preferentially inhibits the growth of SCL-1 cells in a dose- and time-dependent manner, but not of non-malignant keratinocyte HaCaT cells. Acitretin increases the levels of CD95 (Fas), CD95-ligand and Fas-associated death domain. Acitretin is able to induce apoptosis in skin cancer cells possibly via death receptor CD95 apoptosis pathway without affecting the viability of normal keratinocyte. [3]
体内活性
Acitretin undergoes alpha-oxidation, chain shortening O-demethylation, and glucuronidation in the perfused rat liver. [4] Acitretin rapidly appears in liver and muscle of rats, where it undergoes redistribution into skin and adipose tissue. [5]
Cas No.
55079-83-9
分子式
C21H26O3
分子量
326.43
别名
Etretin;Ro 10-1670;阿曲汀;阿维A
储存和溶解度
H2O:<1 mgml
DMSO:16 mg/mL (49 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years