Catalog No.S1368 Synonyms: Etretin, RO 10-1670
Molecular Weight(MW): 326.43
Acitretin is a second generation retinoid used for psoriasis.
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|Description||Acitretin is a second generation retinoid used for psoriasis.|
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. 
|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. |
-  Tippmann F, et al. FASEB J, 2009, 23(6), 1643-1654.
-  Silva FS, et al. Toxicology, 2013, 306, 93-100.
-  Lin XY, et al. J Cell Mol Med, 2009, 13(9A), 2888-2898.
|In vitro||DMSO||20 mg/mL (61.26 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Etretin, RO 10-1670|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02715960||Recruiting||Psoriasis Vulgaris||Central South University||December 2015||Phase 2|
|NCT02050321||Terminated||Malignant Melanoma||University of Arizona||December 2013||Phase 2|
|NCT02330380||Active, not recruiting||Psoriasis|Inflammation||University Hospitals Cleveland Medical Center|National Psoriasis Foundation||April 2013||--|
|NCT01812954||Completed||Psoriasis||Jochen Schmitt.|Merck Sharp & Dohme Corp.|Technische Universität Dresden||March 2013||--|
|NCT02191020||Completed||Psoriasis||Xijing Hospital|Henan Provincial Hospital|The First Affiliated Hospital of Dalian Medical University||February 2013||--|
|NCT01545284||Completed||Chronic Hand Dermatitis||Innovaderm Research Inc.|Tribute Pharmaceuticals||March 2012||Phase 2|Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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