product name Acitretin
Description: Acitretin (also known as Etretin, RO 10-1670) is a second generation retinoid used for psoriasis. Acitretin stimulates ADAM10 promoter activity with an EC50 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. 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.
References: FASEB J. 2009 Jun;23(6):1643-54; Toxicology. 2013 Apr 5;306:93-100; Xenobiotica. 1992 Nov;22(11):1229-37; Drug Metab Dispos. 1994 Jan-Feb;22(1):26-30.
326.43
Formula
C21H26O3
CAS No.
55079-83-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (61.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Etretin, RO 10-1670
other peoduct :
| In Vitro |
In vitro activity: 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. 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. 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. Kinase Assay: Cell Assay: |
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| In Vivo | Acitretin undergoes alpha-oxidation, chain shortening O-demethylation, and glucuronidation in the perfused rat liver. Acitretin rapidly appears in liver and muscle of rats, where it undergoes redistribution into skin and adipose tissue. |
| Animal model | |
| Formulation & Dosage | |
| References | FASEB J. 2009 Jun;23(6):1643-54; Toxicology. 2013 Apr 5;306:93-100; Xenobiotica. 1992 Nov;22(11):1229-37; Drug Metab Dispos. 1994 Jan-Feb;22(1):26-30. |
