Acitretin
作者：齐岳
发布时间：2023-09-13
17:05:59
点击数：
产品名称：Acitretin
产品描述：
| 植物来源 | 天然产物 > 其他（植物来源） > 其他 |
| 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] |
| 别名 | 阿曲汀, 阿维A, Etretin, Ro 10-1670 |
| 分子量 | 326.43 |
| 分子式 | C21H26O3 |
| CAS No. | 55079-83-9 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 16 mg/mL (49 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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