Acitretin

For research use only.

Catalog No.S1368 Synonyms: Etretin, RO 10-1670

2 publications

Acitretin Chemical Structure

CAS No. 55079-83-9

Acitretin (Etretin, RO 10-1670) is a second generation retinoid used for psoriasis.

Selleck's Acitretin has been cited by 2 publications

2 Customer Reviews

  • Acitretin does not induce HIV reactivation in J-lat and ACH-2 cells. (a, b) HIV reactivation induced by acid retinoic (AR) derivative acitretin (25 – 1 μM) in J-Lat cells clone 8.4 (a) and 9.2(b). HDAC inhibitors (HDCAi) panobinostat (PNB, 0.16μM) and vorinostat (VOR, 4 – 0.16 μM) were used as controls. Reactivation was determined by the quantification of GFP+ cells (%) after culturing J-Lat with HDACi and acitretin for 24h. (c, d) HIV reactivation induced by acitretin and HDACi in ACH-2 cells. Reactivation was determined after 48h of incubation by quantification of CAp24 (c) and HIV RNA copy number (d) in the supernatant. Values represent mean±SD of at least three independent experiments performed in triplicate. UN, untreated. *P < 0.05; **P < 0.01; ***P < 0.001.

    Antimicrob Agents Chemother, 2016, 61(11). pii: e01368-17. Acitretin purchased from Selleck.

    Expression of STAT1, pSTAT1, STAT3, pSTAT1, SOCS1 and SOCS3 protein in HaCaT cells of eight groups. HaCaT cells were treated with STAT1-siRNA or STAT3-siRNA (50 nM) in presence or absence of acitretin (5 μM).

    Saudi Pharm J, 2017, 25(4):620-624. Acitretin purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Acitretin (Etretin, RO 10-1670) is a second generation retinoid used for psoriasis.
In vitro

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]

In vivo 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]

Protocol

Solubility (25°C)

In vitro DMSO 20 mg/mL (61.26 mM)
Water Insoluble
Ethanol Insoluble

* 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.

Chemical Information

Molecular Weight 326.43
Formula

C21H26O3

CAS No. 55079-83-9
Storage powder
in solvent
Synonyms Etretin, RO 10-1670
Smiles CC1=CC(=C(C(=C1C=CC(=CC=CC(=CC(=O)O)C)C)C)C)OC

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04841187 Not yet recruiting -- Psoriasis Assistance Publique - Hôpitaux de Paris|Société de Dermatologie Française April 1 2021 --
NCT04245319 Recruiting Drug: Acitretin|Other: Narrow band ultraviolet B Hyperlipidemias|Xerosis|Depression|Liver Diseases Cairo University January 1 2020 Not Applicable
NCT01039142 Completed Drug: Acitretin Psoriasis Postgraduate Institute of Medical Education and Research March 2008 Phase 4
NCT00488384 Withdrawn Drug: Chemopreventive application (Acitretin) Carcinoma Squamous Cell Günther Hofbauer|University of Zurich June 2007 Phase 4
NCT00156247 Completed Drug: acitretin Psoriasis University of Medicine and Dentistry of New Jersey|Connetics Corp.|Rutgers The State University of New Jersey September 2005 Phase 2

Tech Support

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID